C-87 - TNF Receptor 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEC 87Cat. No.: HY-100735CAS No.: 332420-90-3分式: CHClNOS分量: 502.93作靶點(diǎn): TNF Receptor作通路: Apoptosis儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 9.33 mg/mL (18.55 mM; Need ultrasonic and warm

2、ing)H2O : 0.1 mg/mL (insoluble)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.9883 mL 9.9417 mL 19.8835 mL5 mM 0.3977 mL 1.9883 mL 3.9767 mL10 mM 0.1988 mL 0.9942 mL 1.9883 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 C87種新型分TNF抑制劑; 效抑制TNF誘導(dǎo)的細(xì)胞毒性，IC50值為8.73 M。IC50 & Tar

3、get IC50: 8.73 M (TNF-induced cytotoxicity) 1體外研究C87 directly binds to TNF, potently inhibits TNF-induced cytotoxicity (IC50=8.73 M) and effectively blocksTNF-triggered signaling activities. C87 exhibits good solubility and consistent dose-dependent functions in1/2 Master of Small Molecules 您邊的抑制劑師w

4、ww.MedChemEvitro. C87 completely blocks TNF-induced activation of caspase-3 and caspase-8. The activity of c-Jun N-terminal kinase (JNK) is significantly reduced by C87 in L929 cells. C87 also prevents the degradation of IB in cells treated with TNF. C87 potently blocks multiple signaling transducti

5、on pathways and downstreamtarget gene activation triggered by TNF 1.體內(nèi)研究 C87 attenuates TNF-induced inflammation, thereby markedly reducing injuries to the liver and improvinganimal survival. C87 injection delays the incidence of death and increases the survival rate by two foldscompared with the ve

6、hicle control. The level of alanine transaminase and aspartate transaminase isconsistently reduced in mice with C87 treatment 1.PROTOCOLCell Assay 1 The inhibition of the cytotoxic effect of human TNF by compounds (C87) is measured in L929 cell line. L929cells are seeded at a density of 104 cells/we

7、ll in a 96-well plate and incubated for 24 h in RPMI 1640 with10% FBS at 37 C. Compounds (C87) are added to the cells with 1 g/mL actinomycin D and 1 ng/mL TNFand then incubated at 37 C for 20 h before analysis. Cell survival is measured using the MTT method 1.MCE has not independently confirmed the

8、 accuracy of these methods. They are for reference only.Animal BALB/c mice are used in the study. Before LPS/GalN challenge (LPS (50 g/kg) and D-GalN (1.2g/kg), miceAdministration 1 are injected intraperitoneally with C87 (12.5 mg/kg), Enbrel (4 mg/kg), or vehicle, respectively, at 1, 8, and 16h. Bl

9、ood is collected with retro-orbital sampling. Activities of alanine transaminase and aspartatetransaminase are detected. Liver tissues are collected and fixed in 10% formalin, and sections are stainedwith hematoxylin and eosin 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Ma L, et al. A novel small-molecule tumor necrosis factor inhibitor attenuates inflammation in a hepatitis mouse model. J Biol Chem.2014 May 2;289(18):12457-66.McePdfHeightCaution: Product has not been fully validated