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Purity: ≥98%
Mavacamten (also known as SAR439152; MYK461) is a potent and orally bioactive myosin inhibitor with the potential to be used for the treatment of hypertrophic cardiomyopathy/HCM. As of April 28, 2022, Mavacamten (Camzyos, Bristol Myers Squibb) became the first and only FDA-approved allosteric and reversible inhibitor selective for cardiac myosin that targets the underlying pathophysiology of obstructive HCM.
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| ln Vitro |
Mavacamten is shown to have selectivity of >4-fold for cardiac myosin, with IC50 values of 490 nM in the bovine system, 711 nM in the human system, and 2140 nM in the rabbit system[1].
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| ln Vivo |
Mavacamten treatment lowers FS from 52±3% to 38±7%. Mavacamten treatment lowers FS from 81±7% to 60±13%, which is a 25% relative reduction. There is a linear relationship between FS and Mavacamten plasma concentrations across all assays; for every 100 ng/mL rise in Mavacamten concentration, FS is lowered by 4.9%[2]. By lowering the cardiac myosin heavy chain's adenosine triphosphatase activity, mavacamten decreases contractility. In mice with heterozygous human mutations in the myosin heavy chain, chronic Mavacamten treatment inhibits the development of ventricular hypertrophy, cardiomyocyte disarray, and myocardial fibrosis and attenuates hypertrophic and profibrotic gene expression[3].
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| References |
[1]. Kawas RF, et al. A small-molecule modulator of cardiac myosin acts on multiple stages of the myosin chemomechanical cycle. J Biol Chem. 2017 Oct 6;292(40):16571-16577.
[2]. Stern JA, et al. A Small Molecule Inhibitor of Sarcomere Contractility Acutely Relieves Left Ventricular Outflow Tract Obstruction in Feline Hypertrophic Cardiomyopathy. PLoS One. 2016 Dec 14;11(12):e0168407. [3]. Green EM, et al. A small-molecule inhibitor of sarcomere contractility suppresses hypertrophic cardiomyopathy in mice. Science. 2016 Feb 5;351(6273):617-21 |
| Molecular Formula |
C15H19N3O2
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|---|---|
| Molecular Weight |
273.336
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| Exact Mass |
273.1477
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| CAS # |
1642288-47-8
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| Related CAS # |
Mavacamten-d6;2453251-18-6;Mavacamten-d1;2453251-02-8;Mavacamten-d5;2453251-00-6
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| SMILES |
O=C1N(C(C)C)C(C=C(N[C@H](C2=CC=CC=C2)C)N1)=O
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| Chemical Name |
(S)-3-isopropyl-6-((1-phenylethyl)amino)pyrimidine-2,4(1H,3H)-dione
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| Synonyms |
MYK 461SAR-439152 MYK-461 SAR 439152 SAR439152MYK461 Mavacamten
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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 : ~83.33 mg/mL (~304.87 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.15 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 25.0 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 (7.61 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 | 3.6584 mL | 18.2922 mL | 36.5845 mL | |
| 5 mM | 0.7317 mL | 3.6584 mL | 7.3169 mL | |
| 10 mM | 0.3658 mL | 1.8292 mL | 3.6584 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.
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