GPR

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)
カタログ番号	製品カタログ	水	DMSO	アルコール
S4440	2-Phenylacetamide	27 mg/mL	27 mg/mL	''27 mg/mL
S7263	AZD1981	<1 mg/mL	11 mg/mL	<1 mg/mL
S0851	G-1	<1 mg/mL	82 mg/mL	'''<1 mg/mL
S6850	NE 52-QQ57	<1 mg/mL	12 mg/mL	'50 mg/mL
S6651	G15 (GRB-G15)	<1 mg/mL	74 mg/mL	''<1 mg/mL
S0135	JMS-17-2	<1 mg/mL	40 mg/mL	10 mg/mL
S2822	OC000459	<1 mg/mL	4 mg/mL	<1 mg/mL
S0183	NIBR189	<1 mg/mL	42 mg/mL	'''4 mg/mL
S2637	Fasiglifam (TAK-875)	<1 mg/mL	100 mg/mL	<1 mg/mL
S2149	GSK1292263	<1 mg/mL	34 mg/mL	<1 mg/mL
S8014	GW9508	<1 mg/mL	69 mg/mL	69 mg/mL
S0001	GSK137647A	<1 mg/mL	61 mg/mL	'10 mg/mL
S6889	Monomethyl Fumarate	20 mg/mL	26 mg/mL	26 mg/mL
S6746	APD668	<1 mg/mL	96 mg/mL	2 mg/mL
S5400	3-chloro-5-hydroxybenzoic Acid	-1 mg/mL	34 mg/mL	-1 mg/mL
S8673	ONC212	<1 mg/mL	88 mg/mL	88 mg/mL
S0110	APD597	<1 mg/mL	96 mg/mL	<1 mg/mL
S6759	TC-G-1008 (GPR39-C3)	<1 mg/mL	84 mg/mL	2 mg/mL
S6425	JNJ 63533054	-1 mg/mL	63 mg/mL	-1 mg/mL
S0156	CID 1375606	<1 mg/mL	77 mg/mL	<1 mg/mL
S0208	6-OAU	<1 mg/mL	35 mg/mL	<1 mg/mL

GPR製品

All (22) GPR活性剤(1) GPR拮抗剤(7) GPR作動薬(14)

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
S4440^新	2-Phenylacetamide 2-Phenylacetamide, the main compound isolated from the seeds of Lepidium apetalum Willd (LA) with estrogenic activities, increases the expression of Estrogen receptorα (ERα), ERβ and GPR30 in the uterus and MCF-7 cells.
S7263	AZD1981 AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. Phase 2.	Mol Cancer Ther, 2019, 18(11):2097-2110
S0851^新	G-1 G-1 is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM.
S6850^新	NE 52-QQ57 NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).
S6651	G15 (GRB-G15) G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.	Cell Biochem Funct, 2020, 38(1):38-46
S0135	JMS-17-2 JMS-17-2 is a potent and selective small-molecule antagonist of CX3C chemokine receptor 1 (CX3CR1/GPR13) with IC50 of 0.32 nM. JMS-17-2 is used in the research of metastatic disease in breast cancer patients.
S2822	OC000459 OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2.
S0183	NIBR189 NIBR189 is a potent antagonist of the Epstein-Barr virus-induced gene 2 (EBI2, GPR183) receptor with IC50 of 16 nM for binding and 11 nM for function, respectively.
S2637	Fasiglifam (TAK-875) Fasiglifam (TAK-875) is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid.	Endocrinology, 2021, 162(3)bqab002 Psychopharmacology (Berl), 2021, 10.1007/s00213-021-05837-4 Environ Sci Technol, 2020, 54(6):3428-3436	INS-1 cells were incubated with 50 uM palmitate or BSA in the presence or absence of 5 uM TAK 875 for 30 min, followed by stimulation with 16.6 mm [U-13C]glucose for 30 min. Under these conditions, the following were measured: fructose bisphosphate (FBP) (I), NADH/NAD+ ratio (J). Error bars represent mean ?S.E. n = 3-4.
S2149	GSK1292263 GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2.	PLoS One, 2015, 10(7):e0134051	(B) WB403 at 10, 20 μmol/l had no significant stimulation effect on hGPR119 dependent cAMP accumulation. GSK1292263 (1 μmol/l) was used as positive agonist of GPR119.
S8014	GW9508 GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner.	Bioorg Chem, 2020, 99:103830 Arch Pharm (Weinheim), 2020, e2000275 J Pharm Biomed Anal, 2019, 170:176-186
S0001	GSK137647A GSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM.
S6889^新	Monomethyl Fumarate Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.
S6746	APD668 APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.
S5400	3-chloro-5-hydroxybenzoic Acid 3-chloro-5-hydroxybenzoic Acid is a selective agonist of the lactate receptor GPR81.
S8673	ONC212 ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132. ONC212 is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.	Biomolecules, 2020, 10(10)E1395
S0110	APD597 APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).
S6759	TC-G-1008 (GPR39-C3) TC-G-1008 (GPR39-C3) is a potent and orally available G-protein coupled receptor 39 (GPR39)(zinc receptor) agonist with EC50 of 0.4 nM and 0.8 nM for rat and human receptors, respectively.
S6425	JNJ 63533054 JNJ 63533054 is a potent and selective GPR139 agonist. It specifically activated human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays.
S0156	CID 1375606 CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist.
S4709	Latanoprost Latanoprost (Xalatan, PhXA41) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure.
S0208	6-OAU 6-OAU (GTPL5846, 6-n-octylaminouracil) is a surrogate agonist of G protein-coupled receptor 84 (GPR84) that activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with EC50 of 105 nM in the PI assay. 6-OAU (GTPL5846, 6-n-octylaminouracil) increases [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with EC50 of 512 nM.

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

S4440^新

2-Phenylacetamide

2-Phenylacetamide, the main compound isolated from the seeds of Lepidium apetalum Willd (LA) with estrogenic activities, increases the expression of Estrogen receptorα (ERα), ERβ and GPR30 in the uterus and MCF-7 cells.

製品コード	製品説明	文献中Selleckの製品使用例
S7263	AZD1981 AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. Phase 2.	Mol Cancer Ther, 2019, 18(11):2097-2110
S0851^新	G-1 G-1 is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM.
S6850^新	NE 52-QQ57 NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).
S6651	G15 (GRB-G15) G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.	Cell Biochem Funct, 2020, 38(1):38-46
S0135	JMS-17-2 JMS-17-2 is a potent and selective small-molecule antagonist of CX3C chemokine receptor 1 (CX3CR1/GPR13) with IC50 of 0.32 nM. JMS-17-2 is used in the research of metastatic disease in breast cancer patients.
S2822	OC000459 OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2.
S0183	NIBR189 NIBR189 is a potent antagonist of the Epstein-Barr virus-induced gene 2 (EBI2, GPR183) receptor with IC50 of 16 nM for binding and 11 nM for function, respectively.

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
S2637	Fasiglifam (TAK-875) Fasiglifam (TAK-875) is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid.	Endocrinology, 2021, 162(3)bqab002 Psychopharmacology (Berl), 2021, 10.1007/s00213-021-05837-4 Environ Sci Technol, 2020, 54(6):3428-3436	INS-1 cells were incubated with 50 uM palmitate or BSA in the presence or absence of 5 uM TAK 875 for 30 min, followed by stimulation with 16.6 mm [U-13C]glucose for 30 min. Under these conditions, the following were measured: fructose bisphosphate (FBP) (I), NADH/NAD+ ratio (J). Error bars represent mean ?S.E. n = 3-4.
S2149	GSK1292263 GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2.	PLoS One, 2015, 10(7):e0134051	(B) WB403 at 10, 20 μmol/l had no significant stimulation effect on hGPR119 dependent cAMP accumulation. GSK1292263 (1 μmol/l) was used as positive agonist of GPR119.
S8014	GW9508 GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner.	Bioorg Chem, 2020, 99:103830 Arch Pharm (Weinheim), 2020, e2000275 J Pharm Biomed Anal, 2019, 170:176-186
S0001	GSK137647A GSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM.
S6889^新	Monomethyl Fumarate Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.
S6746	APD668 APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.
S5400	3-chloro-5-hydroxybenzoic Acid 3-chloro-5-hydroxybenzoic Acid is a selective agonist of the lactate receptor GPR81.
S8673	ONC212 ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132. ONC212 is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.	Biomolecules, 2020, 10(10)E1395
S0110	APD597 APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).
S6759	TC-G-1008 (GPR39-C3) TC-G-1008 (GPR39-C3) is a potent and orally available G-protein coupled receptor 39 (GPR39)(zinc receptor) agonist with EC50 of 0.4 nM and 0.8 nM for rat and human receptors, respectively.
S6425	JNJ 63533054 JNJ 63533054 is a potent and selective GPR139 agonist. It specifically activated human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays.
S0156	CID 1375606 CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist.
S4709	Latanoprost Latanoprost (Xalatan, PhXA41) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure.
S0208	6-OAU 6-OAU (GTPL5846, 6-n-octylaminouracil) is a surrogate agonist of G protein-coupled receptor 84 (GPR84) that activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with EC50 of 105 nM in the PI assay. 6-OAU (GTPL5846, 6-n-octylaminouracil) increases [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with EC50 of 512 nM.

研究分野別

製品類型

GPR

阻害剤の選択性比較

GPR製品