IMR-1A 是 IMR-1 的酸代谢物,一种有效的 Notch 抑制剂,IC50 为 0.5 μM。IMR-1A 相对于 IMR-1 的效力增加了 50 倍。IMR-1 在体内可以代谢为 IMR-1A。
CAS:331862-41-0
分子式:C13H11NO5S2
分子量:325.36
纯度:98%
存储:Store at -20°C
Background:
IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitors with an IC50 of 0.5 μM. IMR-1A has a 50-fold increase in potency with respect to IMR-1. IMR-1 can metabolize in vivo to IMR-1A[1].
IC50: 0.5 μM (Notch)[1]
IMR-1A (2 mg/kg (i.v.) and 100 mg/kg (i.p)) exhibits low systematic plasma clearance (CL = 7 mL/min/kg) with terminal elimination half-life (T1/2) of 2.22 h following a single i.v. administration. The normal liver blood flow in mice is 90 mL/min/kg and the Vss (volume of distribution) is