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BMS-986224

Catalog No. T39448 CAS 2055200-88-7

Synonyms: BMS 986224

BMS-986224 is an orally active, potent, and selective APJ receptor agonist. BMS-986224 has the potential to study heart failure.

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BMS-986224, CAS 2055200-88-7

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1 mg	In stock	$ 399.00

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Purity: 98.82%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	BMS-986224 is an orally active, potent, and selective APJ receptor agonist. BMS-986224 has the potential to study heart failure.
Targets&IC50	APJ receptor:0.3 nM (Kd), APJ receptor:0.02 nM (EC50, human)
In vitro	Fully inhibits forskolin-mediated cAMP production, with an EC50 for human APJ of 0.02 nM, BMS-986224. BMS-986224 (0-100 nM) fully stimulates β-arrestin recruitment, ERK phosphorylation, and APJ internalization in Chinese hamster ovary-K1 or HEK293 ZF cells. BMS-986224 is a potent and selective APJ receptor agonist that exhibits a similar signaling profile to (Pyr1) apelin-13.
In vivo	In the RHR model, BMS-986224 (0.192 mg/kg or 3 mg/kg; SC infusion; daily) increased stroke volume and cardiac output to levels seen in healthy animals, but without preventing cardiac hypertrophy and fibrosis. These effects are differentiated from enalapril[1].

Synonyms	BMS 986224
Molecular Weight	498.92
Formula	C24H23ClN4O6
CAS No.	2055200-88-7

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (20.04 mM), Sonication is recommended.

References and Literature

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.

Related Products

Related compounds with same targets

ML221 Azelaprag ELA-14(human) acetate [Pyr1]-Apelin-13 (2R,3S)-Azelaprag ELA-11 (human) acetate(1784687-32-6 free base) Apelin-12 acetate CMF019

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Keywords

BMS-986224 2055200-88-7 GPCR/G Protein Apelin receptor BMS986224 BMS 986224 inhibitor inhibit

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