JH-X-119-01 hydrochloride is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 hydrochloride ameliorates LPS-induced sepsis in mice.
体外研究
Jh-X-119-01 (10 μM) decreases phosphorylation of NF-κB and mRNA levels of IL-6 and TNFα in LPS-treated macrophages in vitro. Jh-X-119-01 selectively inhibits IRAK1 phosphorylation.
Western Blot Analysis
Cell Line:
RAW 264.7 cells and THP-1 cells
Concentration:
10 μM
Incubation Time:
15 minutes
Result:
Decreased LPS (100 ng/mL)-induced phosphorylation of IκBα and NF-κB-P65.
体内研究
Jh-X-119-01 improves survival and decreases immunopathies of LPS-challenged mice. Jh-X-119-01 increases survival of mice at the dose of 5 mg/kg body weight. Survival is further improved when the dose is increased to 10 mg/kg.
Animal Model:
C57BL/6 (20-22 g, male) mice
Dosage:
5 mg/kg and 10 mg/kg
Administration:
Intraperitoneally injected; 5 days
Result:
Protected mice from LPS (20 mg/kg)-induced sepsis. Survival at day 5 was 13.3% in control group where septic mice were treated by vehicle, while the values were 37.5% and 56.3% for 5 mg/kg and 10 mg/kg.
分子式
C25H20N6O3.HCl
分子量
488.93
CAS号
2591344-30-6
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 : 50 mg/mL (102.26 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)