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Mavacamten
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
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CAS NO:1642288-47-8
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
MYK-461
SAR439152
产品介绍
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。

产品描述

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

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]

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].

Cas No.

1642288-47-8

分子式

C15H19N3O2

分子量

273.336

别名

MYK-461;SAR439152

储存和溶解度

DMSO:150 mg/mL (548.79 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years