R1487 Hydrochloride is a highly potent and selective p38α inhibitor, with Kd values of 0.2 nM and 29 nM for p38α and p38β, respectively.
IC50&Target
p38α
0.2 nM (Kd)
p38β
29 nM (Kd)
体外研究
R1487 Hydrochloride exhibits IC50 values of 10 nM for p38α inhibition and 200 nM for the inhibition of TNFα induced production of IL-1β.
R1487 (Compounds 2a) inhibits production of TNFα by human monocytic cells (THP-1) and inhibits production of IL-1β in human whole blood (HWB) induced by LPS.
体内研究
R1487 (Compounds 2a, orally) demonstrates significant dose-dependent inhibition of serum TNFα and IL-1β.
Oral bioavailability of 10 mg/kg R1487 (Compounds 2a) in monkey, rat, and dog was 51.6%, 29.3%, 10.3%, respectively.
分子式
C19H18F2N4O3.HCl
分子量
424.83
CAS号
449808-64-4
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 : 20.83 mg/mL (49.03 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)