Inhibitor/Activator
| Cat.No. | Name | Information |
|---|---|---|
| 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. |
| M8281 | 4-CMTB | 4-CMTB is a potent allosteric agonist of free fatty acid receptor 2 (FFA2). |
| 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. |
| M6985 | Monomethyl fumarate | MMF is a activator of Nrf2 pathway; primary metabolite of DMF. |
| M6849 | JNJ 63533054 | JNJ-63533054 is a potent, selective, orally active GPR139 agonist.JNJ-63533054 is more selective for GPR139 than other GPCR, ion channel and transporter proteins.JNJ-63533054 can cross the blood-brain barrier (BBB). |
| M6466 | AS 1269574 | AS1269574 is a potent, orally active GPR119 agonist with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates the TRPA1 cation channel and stimulates glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induced pancreatic β cells to secrete glucose-dependent insulin only under high glucose conditions. AS1269574 has potential for type 2 diabetes research. |
| M6454 | AR420626 | AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, GPR41) with IC50 of 117 nM. |
| M6150 | GPR39-C3 | GPR39-C3 is a potent and orally available GPR39 agonist with EC50 values of 0.4 and 0.8 nM for rat and human receptors respectively. |
| 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). |
| M5292 | GPR120-IN-1 | GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of 7.62. |
| M5187 | GSK137647A | GSK137647A is a selective FFAR4 (GRP120) agonist for human, Mouse and Rat FFA4 with pEC50 values of 6.3, 6.2 and 6.1, respectively. GSK137647A induces insulin secretion and inhibits epithelial ion transport. |
| M5040 | APD597 | APD597 (JNJ-38431055) is a GPR119 agonist used in the study of type 2 diabetes mellitus. The EC50 of hGPR119 is 46 nM. |
| M3950 | APD668 | APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively. APD668 pairs are divided by CYP2C9 (KiNone of the five major CYP subtypes other than =0.1 μM) had no significant inhibitory effect. APD668 can be used for research on steatohepatitis and diabetes. |
| 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. |
| M2091 | OC000459 | OC000459 is a potent, selective, and orally active D prostanoid receptor 2 antagonist. |
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