P450 (e.g. CYP17)

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1123 Abiraterone 0.02 mg/mL 0.1 mg/mL '0.2 mg/mL
S1185 Ritonavir <1 mg/mL 100 mg/mL '''3 mg/mL
S2246 Abiraterone Acetate <1 mg/mL <1 mg/mL 28 mg/mL
S1257 Posaconazole <1 mg/mL 100 mg/mL '<1 mg/mL
S6886 1-Aminobenzotriazole 27 mg/mL 27 mg/mL '27 mg/mL
S3227 5,7-Dimethoxyflavone -1 mg/mL 100 mg/mL ''-1 mg/mL
S6868 Alflutinib (AST2818) mesylate <1 mg/mL 20 mg/mL '''<1 mg/mL
S0230 NVP-VID-400 ˂1 mg/mL 15 mg/mL ˂1 mg/mL
S2187 Avasimibe <1 mg/mL 100 mg/mL ''8 mg/mL
S1353 Ketoconazole <1 mg/mL 5 mg/mL 7 mg/mL
S2476 Itraconazole <1 mg/mL 7 mg/mL ''''<1 mg/mL
S1331 Fluconazole <1 mg/mL 61 mg/mL '61 mg/mL
S1195 TAK-700 (Orteronel) <1 mg/mL 61 mg/mL 8 mg/mL
S2803 Galeterone <1 mg/mL 24 mg/mL 40 mg/mL
S4202 Verapamil HCl 50 mg/mL 98 mg/mL '12 mg/mL
S2555 Clarithromycin <1 mg/mL 25 mg/mL <1 mg/mL
S2900 Cobicistat (GS-9350) <1 mg/mL 100 mg/mL 100 mg/mL
S2496 Ozagrel <1 mg/mL 46 mg/mL <1 mg/mL
S1739 Thiabendazole <1 mg/mL 40 mg/mL 1 mg/mL
S2046 Pioglitazone HCl <1 mg/mL 79 mg/mL ''4 mg/mL
S2067 Ozagrel HCl 52 mg/mL 52 mg/mL 6 mg/mL
S1952 Methoxsalen <1 mg/mL 43 mg/mL '5 mg/mL
S2526 Alizarin <1 mg/mL 48 mg/mL '<1 mg/mL
S1794 Fenofibrate <1 mg/mL 72 mg/mL ''46 mg/mL
S5169 2,6-Dihydroxyanthraquinone -1 mg/mL 48 mg/mL '-1 mg/mL
S2921 PF-4981517 <1 mg/mL 91 mg/mL '<1 mg/mL
S5266 Stiripentol 13 mg/mL 46 mg/mL 46 mg/mL
S5252 Ozagrel sodium 50 mg/mL 1 mg/mL '<1 mg/mL
S2043 Memantine HCl 30 mg/mL 43 mg/mL 43 mg/mL
S9250 Isosilybin -1 mg/mL 97 mg/mL -1 mg/mL
S9257 Acetylshikonin -1 mg/mL 2 mg/mL -1 mg/mL
S2380 Diosmetin <1 mg/mL 60 mg/mL <1 mg/mL
S2262 Apigenin <1 mg/mL 54 mg/mL <1 mg/mL
S4938 Cedrol -1 mg/mL 44 mg/mL -1 mg/mL
S2268 Baicalein <1 mg/mL 54 mg/mL <1 mg/mL
S2389 Naringin Dihydrochalcone <1 mg/mL 100 mg/mL 100 mg/mL
S5416 Metyrapone -1 mg/mL 46 mg/mL -1 mg/mL
S2394 Naringenin <1 mg/mL 54 mg/mL 5 mg/mL
S9299 Ginsenoside F1 -1 mg/mL 100 mg/mL -1 mg/mL
S4963 Purpurin -1 mg/mL 51 mg/mL -1 mg/mL
S3777 Gentiopicroside -1 mg/mL 71 mg/mL -1 mg/mL
S2401 Sodium Danshensu 2 mg/mL 7 mg/mL <1 mg/mL
S3931 Ginsenoside Rd -1 mg/mL 90 mg/mL -1 mg/mL
S4831 Piperonyl butoxide -1 mg/mL 67 mg/mL ''''-1 mg/mL
S3673 Sulfaphenazole <1 mg/mL 62 mg/mL 62 mg/mL
S3917 Tetrahydrocurcumin <1 mg/mL 74 mg/mL 74 mg/mL
S3660 Uniconazole <1 mg/mL 58 mg/mL '58 mg/mL
S2329 Naringin <1 mg/mL 100 mg/mL 2 mg/mL
S4662 Atazanavir <1 mg/mL 71 mg/mL '32 mg/mL
S4221 Benzbromarone <1 mg/mL 85 mg/mL 9 mg/mL
S3719 Topiroxostat <1 mg/mL 40 mg/mL <1 mg/mL
S2344 Piperine <1 mg/mL 57 mg/mL 57 mg/mL
S9442 Bergaptol -1 mg/mL 40 mg/mL -1 mg/mL
S5380 7-Hydroxyflavone -1 mg/mL 47 mg/mL -1 mg/mL
S5529 Galangin <1 mg/mL 54 mg/mL 30 mg/mL
S9241 Polygalaxanthone III -1 mg/mL 100 mg/mL -1 mg/mL
S9163 Rhapontigenin -1 mg/mL 51 mg/mL -1 mg/mL
S2271 Berberine chloride <1 mg/mL 40 mg/mL <1 mg/mL
S4784 Phloracetophenone -1 mg/mL 33 mg/mL -1 mg/mL
S5286 Ramatroban <1 mg/mL 83 mg/mL 83 mg/mL
S2072 Seratrodast(AA-2414) <1 mg/mL 71 mg/mL '7 mg/mL
S6606 CDD3505 <1 mg/mL 2 mg/mL <1 mg/mL
S1442 Voriconazole <1 mg/mL 70 mg/mL ''''20 mg/mL
S6790 Ellipticine hydrochloride ˂1 mg/mL 3 mg/mL ˂1 mg/mL
S1712 Deferasirox <1 mg/mL 74 mg/mL '''2 mg/mL
S4155 Chlorzoxazone <1 mg/mL 34 mg/mL 34 mg/mL
S4741 Danshensu 23 mg/mL <1 mg/mL <1 mg/mL

亜型選択性的な製品

P450 (e.g. CYP17)製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1123

Abiraterone

Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay.

S1185

Ritonavir

Ritonavir (ABT-538, A 84538) is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.

S2246

Abiraterone Acetate

Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay.

S1257

Posaconazole

Posaconazole (SCH56592) is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.

S6886

1-Aminobenzotriazole

1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) is a nonselective and irreversible inhibitor of cytochrome P450 (CYP) enzymes. 1-Aminobenzotriazole is also a substrate and inhibitor of N-acetyltransferase (NAT).

S3227

5,7-Dimethoxyflavone

5,7-Dimethoxyflavone (5,7-DMF) is an inhibitor of cytochrome P450 (CYP) 3As that markedly decreases the expression of CYP3A11 and CYP3A25 in the liver. 5,7-Dimethoxyflavone (5,7-DMF) is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor. 5,7-Dimethoxyflavone (5,7-DMF) is one of the major components of Kaempferia parviflora with anti-obesity, anti-inflammatory, and antineoplastic effects.

S6868

Alflutinib (AST2818) mesylate

Alflutinib (AST2818) mesylate is a third-generation epidermal growth factor receptor (EGFR) inhibitor that inhibits both EGFR-sensitive mutations and T790M mutations. Alflutinib (AST2818), primarily metabolized by CYP3A4, is also a potent CYP3A4 inducer with EC50 of 0.25 μM.

S0230

NVP-VID-400

NVP-VID-400 (SDZ285428) is an inhibitor of CYP51. NVP-VID-400 (SDZ285428) inhibits T. cruzi and T. brucei with I/E2a(5 min) of both <1 and I/E2(60 min) of 9 and 35, respectively.

S2187

Avasimibe

Avasimibe (CI-1011) inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.

S1353

Ketoconazole

Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively.

S2476

Itraconazole

Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.

S1331

Fluconazole

Fluconazole (UK 49858) is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections.

S1195

TAK-700 (Orteronel)

TAK-700 (Orteronel) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). Phase 3.

S2803

Galeterone

Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.

S4202

Verapamil HCl

Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.

S2555

Clarithromycin

Clarithromycin is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections.

S2900

Cobicistat (GS-9350)

Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.

S2496

Ozagrel

Ozagrel is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

S1739

Thiabendazole

Thiabendazole inhibits the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property, used as an anthelmintic and fungicide agent. It is a potent inhibitor of cytochrome P450 1A2 (CYP1A2).

S2046

Pioglitazone HCl

Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.

S2067

Ozagrel HCl

Ozagrel HCl is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

S1952

Methoxsalen

Methoxsalen (Xanthotoxin, NCI-C55903) is a naturally occurring photoactive substance found in the seeds of the Ammi majus (Umbelliferae) plant, used in the diagnosis and treatment of psoriasis; A CYP2A5/6 inhibitor.

S2526

Alizarin

Alizarin (Anthraquinonic) strongly inhibits P450 isoform CYP1A1, CYP1A2 and CYP1B1 with IC50 of 6.2 μM, 10.0 μM and 2.7 μM, respectively; weakly inhibits CYP2A6 and CYP2E1, and does not inhibit CYP2C19, CYP3A4 and CYP3A5.

S1794

Fenofibrate

Fenofibrate (Tricor, Trilipix) is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy.

S5169

2,6-Dihydroxyanthraquinone

2,6-Dihydroxyanthraquinone (Anthraflavic acid, Anthraflavin) is a potent and specific inhibitor of cytochrome P-448 activity.

S2921

PF-4981517

PF-4981517 (CYP3cide, PF-04981517) is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.

S5266

Stiripentol

Stiripentol is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450.

S5252

Ozagrel sodium

Ozagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase inhibitor with neuroprotective properties.

S2043

Memantine HCl

Memantine HCl is a CYP2B6 and CYP2D6 inhibitor for recombinant CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively.

S9250

Isosilybin

Isosilybin is a flavanolignan found in the extract of S. marianum fruits with antioxidant and anticancer activities. Isosilybin inhibits CYP3A4 induction with an IC50 of 74 μM.

S9257

Acetylshikonin

Acetylshikonin is a biologically active compound with anti-cancer and anti-inflammatory activity, which is isolated from the roots of Lithospermum erythrorhizoma. It is a novel general P450 inhibitor with IC50 values of 1.4-4.0 μM for all tested P450s.

S2380

Diosmetin

Diosmetin is a bioflavonoid found in spearmint, oregano, and many other plants.

S2262

Apigenin

Apigenin (NSC 83244, LY 080400) is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM.

S4938

Cedrol

Cedrol, a natural occuring sesquiterpene alcohol, is a potent competitive inhibitor of CYP2B6-mediated bupropion hydroxylase with inhibition constant (Ki) value of 0.9 μM. It also inhibits CYP3A4-mediated midazolam hydroxylation with a Ki value of 3.4 μM while only weakly inhibits CYP2C8, CYP2C9, and CYP2C19 activities.

S2268

Baicalein

Baicalein is a CYP2C9 and prolyl endopeptidase inhibitor.

S2389

Naringin Dihydrochalcone

Naringin Dihydrochalcone(Naringin DC) is a new-style sweetening agent and an artificial sweetener derived from naringin and also an inhibitor of CYP enzymes.

S5416

Metyrapone

Metyrapone is an inhibitor of the enzyme steroid 11-beta-monooxygenase that inhibits adrenal steroid synthesis.

S2394

Naringenin

Naringenin is a natural predominant flavanone derived from plant food, which is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator.

S9299

Ginsenoside F1

Ginsenoside F1, a pharmaceutical component of ginseng, is known to have antiaging, antioxidant, anticancer, and keratinocyte protective effects. Ginsenoside F1 exhibits competitive inhibition of the activity of CYP3A4 with Ki values of 67.8 ± 16.2 μM. Ginsenoside F1 also exhibited a weaker inhibition of the activity of CYP2D6.

S4963

Purpurin

Purpurin is one of the natural colorants extracted from madder roots and other Rubiaceae family plants. It exhibits anti-angiogenic, antifungal, antibiotic, and antioxidative activities.

S3777

Gentiopicroside

Gentiopicroside (GE, Gentiopicrin), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.

S2401

Sodium Danshensu

Sodium Danshensu is a mono sodium of danshensu, which is a natural phenolic acid of caffeic acid derivatives isolated from Salvia miltiorrhiza.

S3931

Ginsenoside Rd

Ginsenoside Rd, a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity.

S4831

Piperonyl butoxide

Piperonyl butoxide (PBO) is a man-made pesticide synergist, working with insect killers to increase their effectiveness.

S3673

Sulfaphenazole

Sulfaphenazole is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).

S3917

Tetrahydrocurcumin

Tetrahydrocurcumin (Tetrahydrodiferuloylmethane, Tetrahydro Curcumin), a major metabolite of curcumin, possesses strong antioxidant and cardioprotective properties.

S3660

Uniconazole

Uniconazole (S 3307D, XE 1019D) is a plant growth regulator that functions by inhibiting cytochrome P450 707As (Ki = 68 nM), a family of enzymes that catabolize ABA. It suppress gibberellin and sterol biosynthesis.

S2329

Naringin

Naringin (Naringoside) is a flavanone glycoside, which exerts a variety of pharmacological effects such as antioxidant activity, blood lipid lowering, anticancer activity, and inhibition of cytochrome P450 enzymes.

S4662

Atazanavir

Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. Atazanavir is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein.

S4221

Benzbromarone

Benzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.

S3719

Topiroxostat

Topiroxostat is a xanthine oxidoreductase (XOR) inhibitor and used for treatment of gout and hyperuricemia.

S2344

Piperine

Piperine (1-Piperoylpiperidine) is the alkaloid responsible for the pungency of black pepper and long pepper, which has also been used in some forms of traditional medicine and as an insecticide.

S9442

Bergaptol

Bergaptol is a natural furanocoumarin found in the essential oils of citrus including lemon and bergamot.Bergaptol is a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 μM.

S5380

7-Hydroxyflavone

7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2. It also has excellent antioxidant properties and great potential to be applied as medicines.

S5529

Galangin

Galangin (3,5,7-trihydroxyflavone; Norizalpinin), a naturally occuring flavonoid found in herbs, is a well-known antioxidant and also an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor.

S9241

Polygalaxanthone III

Polygalaxanthone III is a natural product with the efficacy of tranquilization, glaangal, eliminating sputum and detumescence. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM.

S9163

Rhapontigenin

Rhapontigenin, produced from rhapontin isolated from a methanol extract of Rheum undulatum roots by enzymatic transformation, is a selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM).

S2271

Berberine chloride

Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.

S4784

Phloracetophenone

Phloracetophenone, or 2,4,6-trihydroxyacetophenone (THA), the aglycone component of phloracetophenone glucoside, is a naturally occurring compound obtained from the rhizome of Curcuma comosa (Family Zingiberaceae).

S5286

Ramatroban

Ramatroban (BAY u 3405) is a thromboxane A2(TxA2) receptor antagonist with Ki value of 10 to 13 nM. It also antagonizes a newly identified PGD2 receptor, CRTh2 expressed on the inflammatory cells.

S2072

Seratrodast(AA-2414)

Seratrodast (AA-2414, ABT-001) is a potent and selective thromboxane A2 receptor (TP) antagonist with IC50 of 40 nM used primarily in the treatment of asthma and used as anti-inflammatory agent.

S6606

CDD3505

CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

S1442

Voriconazole

Voriconazole (UK-109496) is a new triazole derivative similar to fluconazole and itraconazole that acts by inhibiting fungal cytochrome P-450-dependent, 14-alpha-sterol demethylase-mediated synthesis of ergosterol.

S6790

Ellipticine hydrochloride

Ellipticine Hydrochloride is a potent inhibitor of DNA topoisomerase II and forms covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases. Ellipticine Hydrochloride is a natural product isolated from the Australian evergreen tree of the Apocynaceae family with antineoplastic activity.

S1712

Deferasirox

Deferasirox (CGP-72670, ICL-670) is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor. Deferasirox-induced iron depletion promotes BclxL downregulation and cell death.

S4155

Chlorzoxazone

Chlorzoxazone is a muscle-relaxing drug,and a probe for human liver cytochrome P-450IIE1.

S4741

Danshensu

Danshensu, a herbal preparation used in traditional Chinese medicine, possesses potential antitumor and anti‑angiogenesis effects.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1123

Abiraterone

Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay.

S1185

Ritonavir

Ritonavir (ABT-538, A 84538) is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.

S2246

Abiraterone Acetate

Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay.

S1257

Posaconazole

Posaconazole (SCH56592) is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.

S6886

1-Aminobenzotriazole

1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) is a nonselective and irreversible inhibitor of cytochrome P450 (CYP) enzymes. 1-Aminobenzotriazole is also a substrate and inhibitor of N-acetyltransferase (NAT).

S3227

5,7-Dimethoxyflavone

5,7-Dimethoxyflavone (5,7-DMF) is an inhibitor of cytochrome P450 (CYP) 3As that markedly decreases the expression of CYP3A11 and CYP3A25 in the liver. 5,7-Dimethoxyflavone (5,7-DMF) is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor. 5,7-Dimethoxyflavone (5,7-DMF) is one of the major components of Kaempferia parviflora with anti-obesity, anti-inflammatory, and antineoplastic effects.

S6868

Alflutinib (AST2818) mesylate

Alflutinib (AST2818) mesylate is a third-generation epidermal growth factor receptor (EGFR) inhibitor that inhibits both EGFR-sensitive mutations and T790M mutations. Alflutinib (AST2818), primarily metabolized by CYP3A4, is also a potent CYP3A4 inducer with EC50 of 0.25 μM.

S0230

NVP-VID-400

NVP-VID-400 (SDZ285428) is an inhibitor of CYP51. NVP-VID-400 (SDZ285428) inhibits T. cruzi and T. brucei with I/E2a(5 min) of both <1 and I/E2(60 min) of 9 and 35, respectively.

S2187

Avasimibe

Avasimibe (CI-1011) inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.

S1353

Ketoconazole

Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively.

S2476

Itraconazole

Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.

S1331

Fluconazole

Fluconazole (UK 49858) is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections.

S1195

TAK-700 (Orteronel)

TAK-700 (Orteronel) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). Phase 3.

S2803

Galeterone

Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.

S4202

Verapamil HCl

Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.

S2555

Clarithromycin

Clarithromycin is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections.

S2900

Cobicistat (GS-9350)

Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.

S2496

Ozagrel

Ozagrel is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

S1739

Thiabendazole

Thiabendazole inhibits the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property, used as an anthelmintic and fungicide agent. It is a potent inhibitor of cytochrome P450 1A2 (CYP1A2).

S2046

Pioglitazone HCl

Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.

S2067

Ozagrel HCl

Ozagrel HCl is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

S1952

Methoxsalen

Methoxsalen (Xanthotoxin, NCI-C55903) is a naturally occurring photoactive substance found in the seeds of the Ammi majus (Umbelliferae) plant, used in the diagnosis and treatment of psoriasis; A CYP2A5/6 inhibitor.

S2526

Alizarin

Alizarin (Anthraquinonic) strongly inhibits P450 isoform CYP1A1, CYP1A2 and CYP1B1 with IC50 of 6.2 μM, 10.0 μM and 2.7 μM, respectively; weakly inhibits CYP2A6 and CYP2E1, and does not inhibit CYP2C19, CYP3A4 and CYP3A5.

S1794

Fenofibrate

Fenofibrate (Tricor, Trilipix) is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy.

S5169

2,6-Dihydroxyanthraquinone

2,6-Dihydroxyanthraquinone (Anthraflavic acid, Anthraflavin) is a potent and specific inhibitor of cytochrome P-448 activity.

S2921

PF-4981517

PF-4981517 (CYP3cide, PF-04981517) is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.

S5266

Stiripentol

Stiripentol is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450.

S5252

Ozagrel sodium

Ozagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase inhibitor with neuroprotective properties.

S2043

Memantine HCl

Memantine HCl is a CYP2B6 and CYP2D6 inhibitor for recombinant CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively.

S9250

Isosilybin

Isosilybin is a flavanolignan found in the extract of S. marianum fruits with antioxidant and anticancer activities. Isosilybin inhibits CYP3A4 induction with an IC50 of 74 μM.

S9257

Acetylshikonin

Acetylshikonin is a biologically active compound with anti-cancer and anti-inflammatory activity, which is isolated from the roots of Lithospermum erythrorhizoma. It is a novel general P450 inhibitor with IC50 values of 1.4-4.0 μM for all tested P450s.

S2380

Diosmetin

Diosmetin is a bioflavonoid found in spearmint, oregano, and many other plants.

S2262

Apigenin

Apigenin (NSC 83244, LY 080400) is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM.

S4938

Cedrol

Cedrol, a natural occuring sesquiterpene alcohol, is a potent competitive inhibitor of CYP2B6-mediated bupropion hydroxylase with inhibition constant (Ki) value of 0.9 μM. It also inhibits CYP3A4-mediated midazolam hydroxylation with a Ki value of 3.4 μM while only weakly inhibits CYP2C8, CYP2C9, and CYP2C19 activities.

S2268

Baicalein

Baicalein is a CYP2C9 and prolyl endopeptidase inhibitor.

S2389

Naringin Dihydrochalcone

Naringin Dihydrochalcone(Naringin DC) is a new-style sweetening agent and an artificial sweetener derived from naringin and also an inhibitor of CYP enzymes.

S5416

Metyrapone

Metyrapone is an inhibitor of the enzyme steroid 11-beta-monooxygenase that inhibits adrenal steroid synthesis.

S2394

Naringenin

Naringenin is a natural predominant flavanone derived from plant food, which is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator.

S9299

Ginsenoside F1

Ginsenoside F1, a pharmaceutical component of ginseng, is known to have antiaging, antioxidant, anticancer, and keratinocyte protective effects. Ginsenoside F1 exhibits competitive inhibition of the activity of CYP3A4 with Ki values of 67.8 ± 16.2 μM. Ginsenoside F1 also exhibited a weaker inhibition of the activity of CYP2D6.

S4963

Purpurin

Purpurin is one of the natural colorants extracted from madder roots and other Rubiaceae family plants. It exhibits anti-angiogenic, antifungal, antibiotic, and antioxidative activities.

S3777

Gentiopicroside

Gentiopicroside (GE, Gentiopicrin), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.

S2401

Sodium Danshensu

Sodium Danshensu is a mono sodium of danshensu, which is a natural phenolic acid of caffeic acid derivatives isolated from Salvia miltiorrhiza.

S3931

Ginsenoside Rd

Ginsenoside Rd, a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity.

S4831

Piperonyl butoxide

Piperonyl butoxide (PBO) is a man-made pesticide synergist, working with insect killers to increase their effectiveness.

S3673

Sulfaphenazole

Sulfaphenazole is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).

S3917

Tetrahydrocurcumin

Tetrahydrocurcumin (Tetrahydrodiferuloylmethane, Tetrahydro Curcumin), a major metabolite of curcumin, possesses strong antioxidant and cardioprotective properties.

S3660

Uniconazole

Uniconazole (S 3307D, XE 1019D) is a plant growth regulator that functions by inhibiting cytochrome P450 707As (Ki = 68 nM), a family of enzymes that catabolize ABA. It suppress gibberellin and sterol biosynthesis.

S2329

Naringin

Naringin (Naringoside) is a flavanone glycoside, which exerts a variety of pharmacological effects such as antioxidant activity, blood lipid lowering, anticancer activity, and inhibition of cytochrome P450 enzymes.

S4662

Atazanavir

Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. Atazanavir is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein.

S4221

Benzbromarone

Benzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.

S3719

Topiroxostat

Topiroxostat is a xanthine oxidoreductase (XOR) inhibitor and used for treatment of gout and hyperuricemia.

S2344

Piperine

Piperine (1-Piperoylpiperidine) is the alkaloid responsible for the pungency of black pepper and long pepper, which has also been used in some forms of traditional medicine and as an insecticide.

S9442

Bergaptol

Bergaptol is a natural furanocoumarin found in the essential oils of citrus including lemon and bergamot.Bergaptol is a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 μM.

S5380

7-Hydroxyflavone

7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2. It also has excellent antioxidant properties and great potential to be applied as medicines.

S5529

Galangin

Galangin (3,5,7-trihydroxyflavone; Norizalpinin), a naturally occuring flavonoid found in herbs, is a well-known antioxidant and also an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor.

S9241

Polygalaxanthone III

Polygalaxanthone III is a natural product with the efficacy of tranquilization, glaangal, eliminating sputum and detumescence. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM.

S9163

Rhapontigenin

Rhapontigenin, produced from rhapontin isolated from a methanol extract of Rheum undulatum roots by enzymatic transformation, is a selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM).

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S2271

Berberine chloride

Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.

2018, 40(3):1525-1532

2014, Haoran Cui

S4784

Phloracetophenone

Phloracetophenone, or 2,4,6-trihydroxyacetophenone (THA), the aglycone component of phloracetophenone glucoside, is a naturally occurring compound obtained from the rhizome of Curcuma comosa (Family Zingiberaceae).

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S5286

Ramatroban

Ramatroban (BAY u 3405) is a thromboxane A2(TxA2) receptor antagonist with Ki value of 10 to 13 nM. It also antagonizes a newly identified PGD2 receptor, CRTh2 expressed on the inflammatory cells.

S2072

Seratrodast(AA-2414)

Seratrodast (AA-2414, ABT-001) is a potent and selective thromboxane A2 receptor (TP) antagonist with IC50 of 40 nM used primarily in the treatment of asthma and used as anti-inflammatory agent.

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S6606

CDD3505

CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

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S1442

Voriconazole

Voriconazole (UK-109496) is a new triazole derivative similar to fluconazole and itraconazole that acts by inhibiting fungal cytochrome P-450-dependent, 14-alpha-sterol demethylase-mediated synthesis of ergosterol.

2020, 6 pii: AAC

2020, 20(1):28

2018, 10.1093/mmy/myx150

S6790

Ellipticine hydrochloride

Ellipticine Hydrochloride is a potent inhibitor of DNA topoisomerase II and forms covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases. Ellipticine Hydrochloride is a natural product isolated from the Australian evergreen tree of the Apocynaceae family with antineoplastic activity.

S1712

Deferasirox

Deferasirox (CGP-72670, ICL-670) is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor. Deferasirox-induced iron depletion promotes BclxL downregulation and cell death.

2019, 14(8):1737-1750

2017, 58(9):1-12

2014, 1;509(7498):105-9.

S4155

Chlorzoxazone

Chlorzoxazone is a muscle-relaxing drug,and a probe for human liver cytochrome P-450IIE1.

S4741

Danshensu

Danshensu, a herbal preparation used in traditional Chinese medicine, possesses potential antitumor and anti‑angiogenesis effects.