S86429 |
CID-2858522 |
| 源叶(MedMol) | 95% |
- 产品描述： CID-2858522 is an effective and specific antigen receptor-mediated NF-κB activation inhibitor (IC50: 70 nM).
- 靶点： NF-κB
- 体内研究： 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
- 细胞实验： Cell viability is estimated based on cellular ATP levels. HEK293 cells at a density of 10^5/mL are seeded at 90 μL per well in 96-well white plates and cultured overnight. Compounds (e.g., CID-2858522; 1 μM, 2 μM, 3 μM, and 4 μM) are added (5 μL in medium) to wells and cells are cultured for 16 h, Finally, 50 μL ATPlite solution is added to each well and luminescence activity is read using a luminometer
- 动物实验： Three male mice are subjected to CID-2858522 (single i.p doses at 10, 30, and 50 mg/kg). Blood is drawn at 0.5 and 3 h, and subsequent LC/MS analysis of pooled samples is performed to determine the overall blood levels of CID-2858522
- 参考文献：
1. Peddibhotla S, et al. Inhibition of protein kinase C-driven nuclear factor-kappaB activation: synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules. J Med Chem. 2010 Jun 24;53(12):4793-7. 2. Okolotowicz KJ, et al. Selective benzimidazole inhibitors of the antigen receptor-mediated NF-kappaB activationpathway. Bioorg Med Chem. 2010 Mar 1;18(5):1918-24.
- 溶解性： Soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.148 ml 10.738 ml 21.476 ml 5 mM 0.43 ml 2.148 ml 4.295 ml 10 mM 0.215 ml 1.074 ml 2.148 ml 50 mM 0.043 ml 0.215 ml 0.43 ml
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