| Bioactivity | 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]. | ||||||||||||
| In Vivo | 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]. | ||||||||||||
| Name | Aficamten | ||||||||||||
| CAS | 2364554-48-1 | ||||||||||||
| Formula | C18H19N5O2 | ||||||||||||
| Molar Mass | 337.38 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |