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描述 | Aficamten (CK-274) is a potent cardiac myosin inhibitor with an IC50 of 1.4 μM, suitable for researching hypertrophic cardiomyopathy (HCM) [1]. |
体内研究 | Aficamten is a next-generation cardiac myosin inhibitor designed for once-daily dosing with a suitable projected human half-life. It reaches a steady state within two weeks and offers a broad therapeutic window in vivo, along with a well-defined pharmacokinetic/pharmacodynamic (PK/PD) relationship [1]. Aficamten shows moderate oral bioavailability following administration, with rates of 98% in mice, 55% to 79% in rats, 45% in dogs, and 41% in monkeys. These figures are based on doses of 1 mg/kg in mice, 2 mg/kg to 8 mg/kg in rats, 1 mg/kg in dogs, and 1 mg/kg in monkeys [1]. Aficamten demonstrates terminal elimination half-lives of 4.5 hours in mice, 3.0 hours in rats, 33.8 hours in dogs, and 8.1 hours in monkeys following intravenous administration at doses of 0.5 mg/kg in mice, 1 mg/kg in rats and dogs, and 1.0 mg/kg in monkeys [1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.96mL 0.59mL 0.30mL |
14.82mL 2.96mL 1.48mL |
29.64mL 5.93mL 2.96mL |
CAS号 | 2364554-48-1 |
分子式 | C18H19N5O2 |
分子量 | 337.376 |
别名 | CK-274;CK-3773274 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 120 mg/mL(355.69 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |