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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 | $213 | In Stock | |
| 5 mg | $538 | In Stock | |
| 10 mg | $793 | In Stock | |
| 25 mg | $1,680 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $589 | 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]. |
| Synonyms | 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) |
| Color | Yellow |
| Appearance | Solid |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 10 mg/mL (20.04 mM), Sonication is recommended. | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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