DRI-C21045是一种有效且选择性的 CD40-CD40L 蛋白-蛋白质相互作用抑制剂,IC50 为 0.17 μM,对 CD40L 诱导的 NF-κB 活化和 B 细胞增殖有浓度依赖性抑制作用,IC50 分别为 17.1 μM 和 4.5 μM。
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描述 | DRI-C21045 is a potent and selective inhibitor of CD40-CD40L costimulatory protein-protein interactions (PPIs) with an IC50 of 0.17 µM. DRI-C21045 showed a concentration-dependent inhibition of both CD40L-induced NF-κB activation and B-cell proliferation, with IC50s of 17.1 µM and 4.5 µM, respectively[1].In the concentration range of 0.6-50 μM for 48 hours, DRI-C21045 blocked CD40L-induced functional activation of primary B cells and inhibited CD40L-induced up-regulation of MHC-II in THP-1 cells. And in the concentration range of 2-100 μM, DRI-C21045 inhibited CD40L-induced B cell proliferation[1]. |
Animal study | At a dose of 30 mg/kg in 20% HPβCD, administered daily by subcutaneous injection, it prolonged graft survival in a murine allogeneic skin transplant model[1].At a dose of 20-60 mg/kg administered by subcutaneous injection twice daily in 20% HPβCD, DRI-C21045 inhibits allogeneic antigen-induced T cell expansion in draining lymph nodes (DLNs)[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.72mL 0.34mL 0.17mL |
8.61mL 1.72mL 0.86mL |
17.22mL 3.44mL 1.72mL |
CAS号 | 2101765-81-3 |
分子式 | C32H24N2O7S |
分子量 | 580.607 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 2 mg/mL(3.44 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |