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BMS-986224 is an orally active, potent, and selective APJ receptor agonist. BMS-986224 has the potential to study heart failure.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $399 | In Stock |
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:0.02 nM (EC50, human), APJ receptor:0.3 nM (Kd) |
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]. |
Alias | BMS 986224 |
Molecular Weight | 498.92 |
Formula | C24H23ClN4O6 |
Cas No. | 2055200-88-7 |
Smiles | CCOCc1[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cn3)o2)c(O)c1-c1c(OC)cccc1OC |
Relative Density. | 1.366 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 10 mg/mL (20.04 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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