Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
Kd: 0.3 nM (APJ receptor)[1]
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ln Vitro |
BMS-986224 has an EC50 of 0.02 nM for human APJ and completely blocks forskolin-mediated cAMP synthesis. Chinese hamster ovary-K1 or HEK293 ZF cells fully respond to BMS-986224 (0-100 nM) in terms of β-arrestin recruitment, ERK phosphorylation, and APJ internalization[1]. Strong and selective APJ receptor agonist BMS-986224 displays a signaling profile resembling that of (Pyr1) apelin-13[1].
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ln Vivo |
In the RHR model, BMS-986224 (0.192 mg/kg or 3 mg/kg; SC infusion; daily) produced effects distinct from enalapril by increasing stroke volume and cardiac output to levels observed in healthy animals, but without preventing cardiac hypertrophy and fibrosis[1].
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Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (renal hypertensive rat model)[1]
Doses: 0.192 mg/kg or 3 mg/kg Route of Administration: SC infusion; daily; Initiated 3 days before surgery and continued for 7 days after surgery Experimental Results: The achieved steady-state plasma concentrations during 10-day infusion were 102 and 2686 nmol/L at low dose and HD, respectively. At the low dose, BMS-986224 increased SV and CO without affecting other measured parameters, including the measured diastolic parameters, cardiac fibrosis, and heart weight in RHR. |
References |
[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.
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Molecular Formula |
C24H23CLN4O6
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Molecular Weight |
498.92
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CAS # |
2055200-88-7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C1(=O)NC(COCC)=C(C2=C(OC)C=CC=C2OC)C(O)=C1C1=NN=C(CC2=NC=C(Cl)C=C2)O1
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 20.83 mg/mL (41.75 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0043 mL | 10.0216 mL | 20.0433 mL | |
5 mM | 0.4009 mL | 2.0043 mL | 4.0087 mL | |
10 mM | 0.2004 mL | 1.0022 mL | 2.0043 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.