| Bioactivity | BMS-986224 is a potent, selective and orally active APJ receptor agonist (Kd = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr1) apelin-13. BMS-986224 has the potential for the research of heart failure[1]. | ||||||||||||
| Target | Kd: 0.3 nM (APJ receptor) | ||||||||||||
| Invitro | BMS-986224 fully inhibits forskolin-mediated cAMP production, with an EC50 for human APJ of 0.02 nM. BMS-986224 (0-100 nM) fully stimulates β-arrestin recruitment, ERK phosphorylation, and APJ internalization in Chinese hamster ovary-K1 or HEK293 ZF cells[1].BMS-986224 is a potent and selective APJ receptor agonist that exhibits a similar signaling profile to (Pyr1) apelin-13[1]. | ||||||||||||
| In Vivo | BMS-986224 (0.192 mg/kg or 3 mg/kg; SC infusion; daily;) in the RHR model increased stroke volume and cardiac output to levels seen in healthy animals but without preventing cardiac hypertrophy and fibrosis, effects differentiated from enalapril[1]. Animal Model: | ||||||||||||
| Name | BMS-986224 | ||||||||||||
| CAS | 2055200-88-7 | ||||||||||||
| Formula | C24H23ClN4O6 | ||||||||||||
| Molar Mass | 498.92 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Gargalovic P, et al. In Vitro and In Vivo Evaluation of a Small-Molecule APJ (Apelin Receptor) Agonist, BMS-986224, as a Potential Treatment for Heart Failure. Circ Heart Fail. 2021;14(3):e007351. |
BMS-986224
CAS: 2055200-88-7 F: C24H23ClN4O6 W: 498.92
BMS-986224 is a potent, selective and orally active APJ receptor agonist (Kd = 0.3 nM). BMS-986224 exhibits similar rece
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