Mavacamten
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MedKoo CAT#: 527002

CAS#: 1642288-47-8

Description: Mavacamten, also known as SAR-439152 and MYK-461, is a myosin inhibitor potentially for the treatment of hypertrophic cardiomyopathy. SAR-439152 reduces contractility by decreasing the adenosine triphosphatase activity of the cardiac myosin heavy chain.

Chemical Structure

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Mavacamten
CAS# 1642288-47-8
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 527002
Name: Mavacamten
CAS#: 1642288-47-8
Chemical Formula: C15H19N3O2
Exact Mass: 273.15
Molecular Weight: 273.336
Elemental Analysis: C, 65.91; H, 7.01; N, 15.37; O, 11.71

Price and Availability

Size Price Availability Quantity
10mg USD 90 Ready to ship
25mg USD 150 Ready to ship
50mg USD 250 Ready to ship
100mg USD 450 Ready to ship
200mg USD 750 Ready to ship
500mg USD 1650 Ready to ship
1g USD 2950 Ready to ship
2g USD 5250 2 weeks
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Synonym: SAR-439152; SAR 439152; SAR439152; MYK-461; MYK 461; MYK461; Mavacamten.

IUPAC/Chemical Name: (S)-3-isopropyl-6-((1-phenylethyl)amino)pyrimidine-2,4(1H,3H)-dione

InChi Key: RLCLASQCAPXVLM-NSHDSACASA-N

InChi Code: InChI=1S/C15H19N3O2/c1-10(2)18-14(19)9-13(17-15(18)20)16-11(3)12-7-5-4-6-8-12/h4-11,16H,1-3H3,(H,17,20)/t11-/m0/s1

SMILES Code: O=C1N(C(C)C)C(C=C(N[C@H](C2=CC=CC=C2)C)N1)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
In vitro activity: TTP (time to peak force) was not significantly affected by 0.33 µM mavacamten treatment but was reduced on average by ∼20% by 0.5 µM mavacamten treatment (P = 0.0021) (Fig. 3E). RT50 was reduced on average by ∼24% by 0.33 µM mavacamten treatment (P = 0.0002) and was further reduced on average by ∼45% by 0.5 µM mavacamten treatment (P = 0.0003) (Fig. 3F). Overall, mavacamten decreased contractility of human engineered heart tissue in a concentration-dependent fashion primarily through decreasing inotropy and increased lusitropy. Reference: Am J Physiol Heart Circ Physiol. 2021 Mar 1;320(3):H1112-H1123. https://pubmed.ncbi.nlm.nih.gov/33449850/
In vivo activity: Treatment of mouse cardiac myofibrils with MYK-461 reduced ATPase activity in a dose-dependent manner [median inhibitory concentration (IC50) of 0.3 µM] (Fig. 1C). Maximal doses of MYK-461 (>10 µM) reduced the maximal ATPase rate by ~90%. Reference: Science. 2016 Feb 5;351(6273):617-21. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4784435/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 33.0 120.73
DMF:PBS (pH 7.2) (1:1) 0.5 1.83
DMSO 52.8 193.08
Ethanol 3.0 10.98

Preparing Stock Solutions

The following data is based on the product molecular weight 273.34 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Sewanan LR, Shen S, Campbell SG. Mavacamten preserves length-dependent contractility and improves diastolic function in human engineered heart tissue. Am J Physiol Heart Circ Physiol. 2021 Mar 1;320(3):H1112-H1123. doi: 10.1152/ajpheart.00325.2020. Epub 2021 Jan 15. PMID: 33449850; PMCID: PMC7988756. 2. Sparrow AJ, Watkins H, Daniels MJ, Redwood C, Robinson P. Mavacamten rescues increased myofilament calcium sensitivity and dysregulation of Ca2+ flux caused by thin filament hypertrophic cardiomyopathy mutations. Am J Physiol Heart Circ Physiol. 2020 Mar 1;318(3):H715-H722. doi: 10.1152/ajpheart.00023.2020. Epub 2020 Feb 21. PMID: 32083971; PMCID: PMC7099453. 3. Stern JA, Markova S, Ueda Y, Kim JB, Pascoe PJ, Evanchik MJ, Green EM, Harris SP. 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. doi: 10.1371/journal.pone.0168407. PMID: 27973580; PMCID: PMC5156432. 4. Green EM, Wakimoto H, Anderson RL, Evanchik MJ, Gorham JM, Harrison BC, Henze M, Kawas R, Oslob JD, Rodriguez HM, Song Y, Wan W, Leinwand LA, Spudich JA, McDowell RS, Seidman JG, Seidman CE. A small-molecule inhibitor of sarcomere contractility suppresses hypertrophic cardiomyopathy in mice. Science. 2016 Feb 5;351(6273):617-21. doi: 10.1126/science.aad3456. PMID: 26912705; PMCID: PMC4784435.
In vitro protocol: 1. Sewanan LR, Shen S, Campbell SG. Mavacamten preserves length-dependent contractility and improves diastolic function in human engineered heart tissue. Am J Physiol Heart Circ Physiol. 2021 Mar 1;320(3):H1112-H1123. doi: 10.1152/ajpheart.00325.2020. Epub 2021 Jan 15. PMID: 33449850; PMCID: PMC7988756. 2. Sparrow AJ, Watkins H, Daniels MJ, Redwood C, Robinson P. Mavacamten rescues increased myofilament calcium sensitivity and dysregulation of Ca2+ flux caused by thin filament hypertrophic cardiomyopathy mutations. Am J Physiol Heart Circ Physiol. 2020 Mar 1;318(3):H715-H722. doi: 10.1152/ajpheart.00023.2020. Epub 2020 Feb 21. PMID: 32083971; PMCID: PMC7099453.
In vivo protocol: 1. Stern JA, Markova S, Ueda Y, Kim JB, Pascoe PJ, Evanchik MJ, Green EM, Harris SP. 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. doi: 10.1371/journal.pone.0168407. PMID: 27973580; PMCID: PMC5156432. 2. Green EM, Wakimoto H, Anderson RL, Evanchik MJ, Gorham JM, Harrison BC, Henze M, Kawas R, Oslob JD, Rodriguez HM, Song Y, Wan W, Leinwand LA, Spudich JA, McDowell RS, Seidman JG, Seidman CE. A small-molecule inhibitor of sarcomere contractility suppresses hypertrophic cardiomyopathy in mice. Science. 2016 Feb 5;351(6273):617-21. doi: 10.1126/science.aad3456. PMID: 26912705; PMCID: PMC4784435.

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1: Green EM, Wakimoto H, Anderson RL, Evanchik MJ, Gorham JM, Harrison BC, Henze M, Kawas R, Oslob JD, Rodriguez HM, Song Y, Wan W, Leinwand LA, Spudich JA, McDowell RS, Seidman JG, Seidman CE. A small-molecule inhibitor of sarcomere contractility suppresses hypertrophic cardiomyopathy in mice. Science. 2016 Feb 5;351(6273):617-21. doi: 10.1126/science.aad3456. PubMed PMID: 26912705; PubMed Central PMCID: PMC4784435.