化合物MYK-461 T7134

Product Introduction
Bioactivity


英文名: Mavacamten

描述: Mavacamten (MYK-461) 是一种可口服的心肌肌球蛋白 ATP 酶抑制剂，在牛心脏和人心脏中的IC50值分别为 490和711 nM。

动物实验: 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].

体外活性: 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]

体内活性: MYK-461 reduces cardiac contractility, prevents left ventricular hypertrophy, and reverses pathologic remodeling. In cats, it relieves left ventricular outflow tract obstruction[2]

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

溶解度: DMSO : 150 mg/mL (548.79 mM)


关键字: Myosin | Inhibitor | inhibit | Mavacamten | MYK 461 | SAR-439152 | SAR 439152 | MYK461

相关产品: Danicamtiv | JB062 | para-Nitroblebbistatin | JB002 | (-)-Blebbistatin | Phenamacril | Omecamtiv mecarbil | ML-7 hydrochloride | 16-38-Thymosin β4 (cattle) (TFA) | Myosin V-IN-1

相关库: Drug Repurposing Compound Library | Approved Drug Library | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compounds Library Max | Inhibitor Library | Cytoskeletal Signaling Pathway Compound Library | EMA Approved Drug Library | Orally Active Compound Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compound Library

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