IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitor 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.
体内研究
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 ~4-fold. Plasma concentrations is quantifiable up to 24 h with Tmax of 0.50 h after i.p. administration.
Animal Model:
Male C57 BL/6 mice
Dosage:
2 mg/kg (i.v.) and 100 mg/kg (i.p)
Administration:
I.v. and i.p.
Result:
Exhibited 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 and plasma concentrations is quantifiable up to 24 h with Tmax of 0.50 h after i.p. administration.
分子式
C13H11NO5S2
分子量
325.36
CAS号
331862-41-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 2 mg/mL (6.15 mM; Need ultrasonic)
H2O : 1 mg/mL (3.07 mM; ultrasonic and warming and heat to 80°C)