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MYK-461 (Mavacamten) Cardiac Myosin Modulator

Name: MYK-461 (Mavacamten)
Brand: Selleck Chemicals
SKU: S8861
Availability: InStock
Rating: 5 (6 reviews)

Cat.No.S8861

Mavacamten (MYK-461, SAR439152) is a small-molecule modulator of cardiac myosin that targets the underlying sarcomere hypercontractility of hypertrophic cardiomyopathy (HCM), one of the most prevalent heritable cardiovascular disorders.

Chemical Structure

Molecular Weight: 273.33

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Quality Control

Batch: Purity: 99.92%

99.92

Related Targets	Akt Wnt/beta-catenin HSP PKC ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK
Other Cardiac Myosin Inhibitors	Danicamtiv (MYK-491) CK-586 Aficamten (CK-274)

Solubility

In vitro
Batch:

DMSO : 55 mg/mL (201.22 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.350mg/ml (4.94mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.220mg/ml (0.80mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	273.33	Formula	C₁₅H₁₉N₃O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1642288-47-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	SAR439152			Smiles	CC(C)N1C(=O)C=C(NC1=O)NC(C)C2=CC=CC=C2

Mechanism of Action

In vitro	Mavacamten (MYK-461) primarily reduces the steady-state ATPase activity by inhibiting the rate of phosphate release of β-cardiac myosin-S1. This compound modulates multiple steps of the myosin chemomechanical cycle. In addition to decreasing the rate-limiting step of the cycle (phosphate release), it reduces the number of myosin-S1 heads that can interact with the actin thin filament during transition from the weakly to the strongly bound state without affecting the intrinsic rate. It also decreases the rate of myosin binding to actin in the ADP-bound state and the ADP-release rate from myosin-S1 alone.
In vivo	In mice harboring heterozygous human mutations in the myosin heavy chain, early, chronic administration of Mavacamten (MYK-461) suppresses the development of ventricular hypertrophy, cardiomyocyte disarray, and myocardial fibrosis and attenuates hypertrophic and profibrotic gene expression.
References	[1] https://pubmed.ncbi.nlm.nih.gov/28808052/ [2] https://pubmed.ncbi.nlm.nih.gov/26912705/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06338202	Not yet recruiting	Obstructive Hypertrophic Cardiomyopathy (oHCM)	Bristol-Myers Squibb	April 1 2024	--
NCT06253221	Recruiting	Cardiomyopathy Hypertrophic	Bristol-Myers Squibb	April 17 2024	Phase 3
NCT06023186	Not yet recruiting	Obstructive Hypertrophic Cardiomyopathy	Michael Ayers\|Bristol-Myers Squibb\|University of Virginia	September 15 2023	--
NCT05489705	Recruiting	Obstructive Hypertrophic Cardiomyopathy	Bristol-Myers Squibb	August 16 2022	--
NCT04766892	Active not recruiting	Heart Failure With Preserved Ejection Fraction	Bristol-Myers Squibb	March 30 2021	Phase 2

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