CID-2858522
CID-2858522 性质
沸点 | 618.9±65.0 °C(Predicted) |
---|---|
密度 | 1.12±0.1 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | DMSO:可溶,2mg/mL,澄清(加热) |
酸度系数(pKa) | 8.46±0.40(Predicted) |
形态 | 粉末 |
颜色 | 白色至米色 |
CID-2858522 用途与合成方法
NF-κB 70 nM (IC 50 ) |
CID-2858522 (Compound 1) inhibits antigen receptor-mediated NF-κB with an IC 50 of 70 nM. CID-2858522 also inhibits testosterone hydroxylase in the presence of human liver microsomes (HLM) and an NADPH generating system with an IC 50 of 85 μM. In the HEK293 cell line used for primary screening, CID-2858522 suppresses NF-κB reporter gene activity in a concentration-dependent manner, with IC 50 ~70 nM and with maximum inhibition achieved at 0.25-0.5 μM. In contrast, CID-2858522 does not inhibit TNF-induced NF-κB-reporter gene activity at concentrations as high as 4 μM, thus demonstrating selectivity for the NF-κB pathway activated by PMA/Ionomycin. Cell viability assays indicate that CID-2858522 is not toxic to HEK293 cells at concentrations ≤8 μM. CID-2858522 also potently inhibits PMA/Ionomycin-induced NF-κB reporter gene activity in transient transfection assays.
In vivo dose-exposure profiling of CID-2858522 (Compound 1a) is conducted using a small cohort of three male mice. CID-2858522 exhibits nonlinear pharmacokinetics, showing higher serum levels at the 0.5 h measurement time for the 30 mg/kg dose compared to 50 mg/kg but displaying typical dose-dependent behavior when measured at t=3 h. The increasing accumulation seen at a dose of 50 mg/kg may be due to a depot effect created by CYP3A4 inhibition. The cohort exhibits clear signs of morbidity at t=3 h at the 50 mg/kg dose.
1-[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-[2-[(3-hydroxypropyl)amino]-5,6-dimethyl-1H-benzimidazol-1-yl]-ethanone is a selective benzimidazole inhibitor of the antigen receptor-mediated NF-κB a ctivation pathway.
CID-2858522 价格(试剂级)
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024-11-08 | HY-15530 | CID-2858522 | 1 mg | 340 | |
2024-11-08 | HY-15530 | CID-2858522 | 758679-97-9 | 5mg | 835 |