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Aficamten
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。
Aficamten图片
CAS NO:2364554-48-1
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
Aficamten (CK-274) 是一种新型心肌肌球蛋白 (cardiac myosin)抑制剂,IC50 为 1.4 μM。Aficamten 可用于肥厚型心肌病 (HCM) 的研究。
Cas No.2364554-48-1
别名CK-274; CK-3773274
分子式C18H19N5O2
分子量337.38
溶解度DMSO : 125 mg/mL (370.50 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Aficamten (CK-274) is a potent cardiac myosin inhibitor with an IC50 of 1.4 μM. Aficamten can be used for the research of hypertrophic cardiomyopathy (HCM)[1].

Aficamten is a next-generation cardiac myosin inhibitor that provides a projected human half-life appropriate for once a day dosing, reaching steady state within two weeks, and demonstrates a wide therapeutic window in vivo with a clear PK/PD relationship[1]. Aficamten exhibits moderate oral bioavailability (mouse 98%, rat 55%, rat 58%,rat 79%, dog 45%, monkey 41%) following oral administration (mouse 1 mg/kg, rat 2 mg/kg, rat 3 mg/kg, rat 8 mg/kg, dog 1 mg/kg and monkey 1 mg/kg)[1].Aficamten exhibits terminal elimination half-lives (mouse 4.5 h, rat 3.0 h, dog 33.8 h and, monkey 8.1 h) following intravenous administration (mouse 0.5 mg/kg, rat 1 mg/kg, dog 1 mg/kg and monkey 1.0 mg/kg)[1].

[1]. Chihyuan Chuang, et al. Discovery of Aficamten (CK-274), a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy. J Med Chem. 2021 Oct 14;64(19):14142-14152.