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。
货号:ajcx35840
CAS:2364554-48-1
分子式:C18H19N5O2
分子量：337.38
溶解度:DMSO : 125 mg/mL (370.50 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.