Inhibitor/Activator
| Cat.No. | Name | Information |
|---|---|---|
| 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. |
| M3916 | Vincamine | Vincamine can be used as a peripheral vascular dilator (Vasodilator) to selectively regulate cerebral microvascular circulation. Vincamine is a GPR40 agonist that plays a beta-cell protective role by improving beta-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine can improve glucose homeostasis in vivo and has potential in the study of type 2 diabetes (T2DM). |
| 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. |
| M2054 | Fasiglifam (TAK-875) Hemihydrate | Fasiglifam (TAK-875) Hemihydrate is a novel, orally available, selective GPR40 agonist. |
| M2020 | GW9508 | GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 has anti-inflammatory and anti-atherosclerotic activities. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. |
| M54438 | [Ala17]-MCH | [Ala17]-MCH, a MCH analogue, is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). |
| M54286 | BigLEN(rat) | BigLEN(rat) is a potent GPR171 agonist with an EC50 of 1.6 nM. |
| M53855 | BigLEN(mouse) | BigLEN(mouse) is a potent and selective agonist of orphan G protein-coupled receptor 171 (GPR171), with a Kd of ∼0.5 nM. |
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