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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| 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. |
| M2091 | OC000459 | OC000459 is a potent, selective, and orally active D prostanoid receptor 2 antagonist. |
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