C 87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.
体外研究
C 87 (C87) directly binds to TNFα, potently inhibits TNFα-induced cytotoxicity (IC50=8.73 μM) and effectively blocks TNFα-triggered signaling activities. C 87 exhibits good solubility and consistent dose-dependent functions in vitro. C 87 completely blocks TNFα-induced activation of caspase-3 and caspase-8. The activity of c-Jun N-terminal kinase (JNK) is significantly reduced by C 87 in L929 cells. C 87 also prevents the degradation of IκBα in cells treated with TNFα. C 87 potently blocks multiple signaling transduction pathways and downstream target gene activation triggered by TNFα.
体内研究
C 87 (C87) attenuates TNFα-induced inflammation, thereby markedly reducing injuries to the liver and improving animal survival. C 87 injection delays the incidence of death and increases the survival rate by two folds compared with the vehicle control. The level of alanine transaminase and aspartate transaminase is consistently reduced in mice with C 87 treatment.
分子式
C24H15ClN6O3S
分子量
502.93
CAS号
332420-90-3
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 : 9.33 mg/mL (18.55 mM; Need ultrasonic and warming)