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Chemical Structure : BMS-986224
CAS No.: 2055200-88-7
Catalog No.: PC-38138Not For Human Use, Lab Use Only.
BMS-986224 (BMS986224) is a novel potent, selective, orally bioavailable agonist of Apelin receptor (APJ, APLNR) with Ki of 0.074 nM (human APJ).
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|---|---|---|---|
| 5 mg | $498 | In stock | |
| 10 mg | $788 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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BMS-986224 (BMS986224) is a novel potent, selective, orally bioavailable agonist of Apelin receptor (APJ, APLNR) with Ki of 0.074 nM (human APJ).
BMS-986224 is highly selective for the APJ receptor and did not bind other GPCRs at 30 uM concentration.
BMS-986224 showed to be a fully competitive and high-affinity orthosteric ligand, displacing (Pyr1) apelin-13 from the human APJ receptor.
BMS-986224 inhibited forskolin-mediated cAMP production (EC50=0.02 nM), stimulate β-arrestin recruitment, increase ERK phosphorylation, and induce receptor internalization, and EC50 values for monkey, dog, rat, and mouse APJ were similar.
BMS-986224 induces a sustained increase in cardiac output in the cardiac disease setting and exhibits a differentiated profile from the renin-angiotensin system inhibitor enalapril.
| M.Wt | 498.92 | |
| Formula | C24H23ClN4O6 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
3-(5-((5-chloropyridin-2-yl)methyl)-1,3,4-oxadiazol-2-yl)-5-(2,6-dimethoxyphenyl)-6-(ethoxymethyl)-4-hydroxypyridin-2(1H)-one |
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1. Gargalovic P, et al. Circ Heart Fail. 2021 Mar;14(3):e007351.
2. Pi Z, et al. ACS Med Chem Lett. 2021 Oct 22;12(11):1766-1772.
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