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Mavacamten

Catalog No. T7134   CAS 1642288-47-8
Synonyms: MYK-461, SAR439152

Mavacamten (MYK-461) is an orally bioavailable inhibitor of cardiac myosin ATPase,( IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively)

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Mavacamten Chemical Structure
Mavacamten, CAS 1642288-47-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 55.00
5 mg In stock $ 97.00
10 mg In stock $ 133.00
25 mg In stock $ 271.00
50 mg In stock $ 450.00
100 mg In stock $ 657.00
1 mL * 10 mM (in DMSO) In stock $ 172.00
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Mavacamten (MYK-461) is an orally bioavailable inhibitor of cardiac myosin ATPase,( IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively)
Targets&IC50 human cardiac:711 nM, bovine cardiac:490 nM
In vitro MYK-461 is found to have an IC50 value of 490 nM in the bovine system, 711 nM in the human system, and 2140 nM in the rabbit system, indicating selectivity of >4-fold for cardiac myosin[1]
In vivo MYK-461 reduces cardiac contractility, prevents left ventricular hypertrophy, and reverses pathologic remodeling. In cats, it relieves left ventricular outflow tract obstruction[2]
Animal Research Five?cats received a combination of alfaxalone and midazolam for anesthetic induction, followed by inhaled isoflurane and oxygen maintenance.?Blood pressure was measured via an automated blood pressure cuff at five-minute intervals with supplementary continuous monitoring by arterial line when arterial access could be obtained.?Following induction of anesthesia, a complete baseline echocardiogram was performed (timepoint #1).?Cats were then treated with atropine 0.04 mg/kg IV, followed by an infusion of isoproterenol 0.04 μg/kg/min IV to elevate heart rate back to pre-anesthetized values and induce the previously observed LVOT obstruction.?After five to seven minutes, a stable heart rate of 200–220 bpm was reached and a complete echocardiogram was performed (timepoint #2).?At the completion of imaging, a ten-minute intravenous infusion of MYK-461 (n = 5) at 0.3 mg/kg/hr IV was started.?Focused echocardiography was performed after five minutes (timepoint #3).?After ten minutes, the MYK-461 infusion rate was lowered to 0.12 mg/kg/hr IV, a blood sample was drawn and an echocardiogram performed (timepoint #4).?If ventricular function remained hypercontractile or within normal limits by visual inspection, another blood sample was obtained and the MYK-461infusion rate was increased to 0.36 mg/kg/hr IV for ten minutes.?Focused echocardiography was performed after five minutes (timepoint #5).?After ten minutes, the MYK-461 infusion rate was lowered to 0.15 mg/kg/hr IV, a blood sample was drawn and an echocardiogram performed (timepoint #6).?Following imaging, the isoproterenol infusion was discontinued.?When heart rate returned to baseline levels (five to seven minutes), a complete echocardiogram was performed on MYK-461 alone (timepoint #7).?Study drug was then discontinued, and animals were awakened, extubated and moved to recovery.?Three of five cats were available to return for a control arm of this experiment after a 6-week washout period.The experiment was completed with identical methodology with the exception that MYK-461 was substituted for vehicle (control) at matched volumes/infusion rates[2].
Synonyms MYK-461, SAR439152
Molecular Weight 273.33
Formula C15H19N3O2
CAS No. 1642288-47-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 150 mg/mL (548.79 mM)

TargetMolReferences and Literature

1. Kawas R F , Anderson R L , Ingle S R B , et al. A small molecule modulator of cardiac myosin acts on multiple stages of the myosin chemomechanical cycle[J]. Journal of Biological Chemistry, 2017, 292(40):jbc.M117.776815. 2. Stern J A , Markova S , Ueda Y , et al. A Small Molecule Inhibitor of Sarcomere Contractility Acutely Relieves Left Ventricular Outflow Tract Obstruction in Feline Hypertrophic Cardiomyopathy[J]. Plos One, 2016, 11(12):e0168407.

Related compound libraries

This product is contained In the following compound libraries:
FDA-Approved Drug Library Bioactive Compounds Library Max Clinical Compound Library Inhibitor Library Drug Repurposing Compound Library FDA-Approved & Pharmacopeia Drug Library Orally Active Compound Library Cytoskeletal Signaling Pathway Compound Library Bioactive Compound Library NO PAINS Compound Library

Related Products

Related compounds with same targets
JB061 Blebbistatin 16-38-Thymosin β4 (cattle) (TFA) Myosin V-IN-1 JB062 ML-7 hydrochloride JB002 W-7 hydrochloride

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Keywords

Mavacamten 1642288-47-8 Cytoskeletal Signaling Myosin Inhibitor inhibit MYK-461 MYK 461 SAR439152 SAR-439152 SAR 439152 MYK461 inhibitor

 

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