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)
DMSO アルコール
S7263 AZD1981 <1 mg/mL 11 mg/mL <1 mg/mL
S6850 NE 52-QQ57 <1 mg/mL 12 mg/mL ''50 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
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
S6746 APD668 <1 mg/mL 96 mg/mL 2 mg/mL
S6889 Monomethyl Fumarate 20 mg/mL 26 mg/mL '''26 mg/mL
S0156 CID 1375606 <1 mg/mL 77 mg/mL '''<1 mg/mL
S6759 TC-G-1008 (GPR39-C3) <1 mg/mL 84 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
S6425 JNJ 63533054 -1 mg/mL 63 mg/mL ''-1 mg/mL
S4709 Latanoprost ' mg/mL

GPR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
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.

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).

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.

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.

S2149

GSK1292263

GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2.

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.

S6746

APD668

APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.

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.

S0156

CID 1375606

CID 1375606 is an orphan G protein-coupled receptor GPR27 agonist.

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.

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.

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.

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.

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
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.

2019, 18(11):2097-2110

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).

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.

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.

2020, 54(6):3428-3436

2018, 159(8):2939-2952

2017, 7(1):4657

S2149

GSK1292263

GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2.

2015, 10(7):e0134051

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.

2020, 99:103830

2019, 170:176-186

2018, 32(7):3924-3935

S6746

APD668

APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.

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.

S0156

CID 1375606

CID 1375606 is an orphan G protein-coupled receptor GPR27 agonist.

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.

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.

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.

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.