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Postion:Product Catalog >API>Inhibitors>Mavacamten
Mavacamten
  • Mavacamten

Mavacamten NEW

Price $40 $73 $108
Package 1mg 5mg 10mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: Mavacamten CAS No.: 1642288-47-8
Purity: 99.53% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameMavacamten
DescriptionMavacamten (MYK-461) is an orally bioavailable inhibitor of cardiac myosin ATPase,( IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively)
Animal ResearchFive?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].
In vitroMYK-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 vivoMYK-461 reduces cardiac contractility, prevents left ventricular hypertrophy, and reverses pathologic remodeling. In cats, it relieves left ventricular outflow tract obstruction[2]
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 150 mg/mL (548.79 mM)
KeywordsMyosin | Inhibitor | inhibit | Mavacamten | MYK 461 | SAR-439152 | SAR 439152 | MYK461
Inhibitors RelatedMyosin V-IN-1 | JB062 | Phenamacril | JB002 | Danicamtiv | Blebbistatin | HA-100 | ATM-3507 | ML-7 hydrochloride | JB061 | ML-9 | BTS
Related Compound LibrariesBioactive Compound Library | Approved Drug Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | FDA-Approved Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Cytoskeletal Signaling Pathway Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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