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
S9477	AH7614	<1 mg/mL	70 mg/mL	''<1 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
S6850	NE 52-QQ57	<1 mg/mL	12 mg/mL	'50 mg/mL
S2822	OC000459	<1 mg/mL	4 mg/mL	<1 mg/mL
S0183	NIBR189	<1 mg/mL	42 mg/mL	'''4 mg/mL
S0851	G-1	<1 mg/mL	82 mg/mL	'''<1 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
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
S6889	Monomethyl Fumarate	20 mg/mL	26 mg/mL	26 mg/mL
S0208	6-OAU	<1 mg/mL	35 mg/mL	<1 mg/mL

GPR製品

All (23) GPR活性剤(1) GPR拮抗剤(8) 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
S9477^新	AH7614 AH7614 (compound 39) is a selective FFA4 (GPR120) antagonist with pIC50s of 7.1 for human FFA4 and 8.1 for mouse FFA4.
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.
S6850	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).
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.
S0851	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.
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.	J Enzyme Inhib Med Chem, 2021, 36(1):1651-1658 Bioorg Chem, 2020, 99:103830 Arch Pharm (Weinheim), 2020, e2000275
S0001	GSK137647A GSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM.
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.
S6889	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.	Aging (Albany NY), 2021, 13(13):17097-17117
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
S9477^新	AH7614 AH7614 (compound 39) is a selective FFA4 (GPR120) antagonist with pIC50s of 7.1 for human FFA4 and 8.1 for mouse FFA4.
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.
S6850	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).
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.
S0851	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.

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.	J Enzyme Inhib Med Chem, 2021, 36(1):1651-1658 Bioorg Chem, 2020, 99:103830 Arch Pharm (Weinheim), 2020, e2000275
S0001	GSK137647A GSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM.
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.
S6889	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.	Aging (Albany NY), 2021, 13(13):17097-17117
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