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
S0001 GSK137647A <1 mg/mL 61 mg/mL ''10 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
S0156 CID 1375606 <1 mg/mL 77 mg/mL ''''<1 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
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
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.

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

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.

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.

S0156

CID 1375606

CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist.

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.

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.

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

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

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.

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.

S0156

CID 1375606

CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist.

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.

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.

2020, 10(10)E1395

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.