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GPR G protein-coupled receptor

Inhibitors

Cat.No.  Name Information
M20180 WAY-388798 WAY-388798 is a agonist of free fatty acid receptor 1 (GPR40)
M10634 NE 52-QQ57 NE 52-QQ57 is an orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 significantly inhibited 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).
M10562 GPR81 agonist 1 GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC50 values of 58 nM and 50 nM for human and mouse GPR81, respectively.
M10469 MCH TFA (human, mouse, rat) MCH TFA (human, mouse, rat) is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively.
M9494 AF64394 AF64394 is a selective GPR3 inverse agonist with a pIC50 of 7.3.
M9245 GTPL5846 GTPL5846 (6-OAU) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.
M8948 TUG-891 TUG-891 is a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120).
M7541 TUG-770 Tug-770 is a potent, selective, orally active GPR40/FFA1 agonist with an EC50 of 6 nM against human FFA1. Tug-770 has higher selectivity to FFA1 than FFA2, FFA3, FFA4, PPARγ, other receptors, transporters and enzymes.
M6257 ONC212 ONC212, a fluorinated-ONC201 analogue, is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.
M6141 NIBR189 NIBR189 is a small molecule antagonist of the Epstein-Barr virus-induced gene 2 (EBI2; GPR183) receptor with IC50 of 16 nM(Binding) and 11 nM (Functional).
M5729 Latanoprost Latanoprost 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.
M5292 GPR120-IN-1 GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of 7.62.
M5187 GSK137647A GSK137647A is a selective FFA4 agonist for human, Mouse and Rat FFA4 with pEC50 values of 6.3, 6.2 and 6.1, respectively.
M3773 PSN-375963 PSN 375963 is an effective GPR119 agonist with EC50 of 8.4 and 7.9 μM for human and mice, respectively. PSN 375963 showed similar potency to endogenous oleoylethanolamide (OEA).
M3771 PSN632408 PSN632408 is a novel, selective and small-molecule agonist of human and mouse GPR119 with EC50 values of 5.6±0.99 μM and 7.9±0.7 μM, respectively.
M3766 AR-231453 AR-231453 is a potent, selective G-protein coupled receptor 119 (GPR119) agonist (EC50 = 0.68 nM).
M3632 MBX-2982 MBX-2982 is a selective, orally-available GPR119 agonist for the treatment of type 2 diabetes.
M3321 GSK1292263 GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes.
M2418 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.
M2384 AMG-837 AMG 837 is a potent, orally bioavailable GPR40 agonist with EC50 of 14 nM.



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