DRI-C21045 (compound 10) 是一种有效和选择性的CD40-CD40L共刺激蛋白-蛋白质相互作用 (PPI) 抑制剂，IC50为 0.17 μM。DRI-C21045 显示对 CD40L 诱导的 NF-κB 活化和 B 细胞增殖的浓度依赖性抑制，IC50分别为 17.1 μM 和 4.5 μM。
| 生物活性 | DRI-C21045 (compound 10) is a potent and selective inhibitor of theCD40-CD40Lcostimulatory protein-protein interaction (PPI) with anIC50of 0.17 μM. DRI-C21045 shows concentration-dependent inhibition of the activation ofNF-κBand B cell proliferation all induced by CD40L with IC50s of 17.1 μM and 4.5 μM, respectively[1]. |
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体外研究
(In Vitro) | DRI-C21045 (3.2-100 μM; 18 h) concentration-dependently inhibits the CD40L-induced NF-κB activation in CD40 sensor cells[1].
DRI-C21045 (0.6-50 μM; 48 h) blocks CD40L-induced functional activation of primary B cells[1].
DRI-C21045 (0.4-50 μM; 48 h) inhibits CD40L-induced MHC-II upregulation in THP-1 cells[1].
DRI-C21045 (2-100 μM; 48 h) inhibits CD40L-induced B cell proliferation[1].
DRI-C21045 shows no signs of cytotoxicity for concentrations of up to 100 and 200 μM and has no genotoxic potential for concentrations of up to 500 μM[1].
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体内研究
(In Vivo) | DRI-C21045 (30 mg/kg; daily, s.c.; in 20% HPβCD) prolongs graft survival in a murine allogeneic skin transplant model[1].
DRI-C21045 (20-60 mg/kg; twice daily s.c.; in 20% HPβCD) inhibits alloantigen-induced T cell expansion in the draining lymph nodes (DLNs)[1].
| Animal Model: | Full-thickness ear skins from BALB/c were transplanted onto the dorsal thorax of C57BL/6[1] | | Dosage: | 30 mg/kg | | Administration: | Daily s.c; administered in 20% w/v hydroxypropyl-β-cyclodextrin (HPβCD) solution | | Result: | Caused prolongation of skin allograft survival. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 2 mg/mL(3.44 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.7223 mL | 8.6116 mL | 17.2233 mL | | 5 mM | --- | --- | --- | | 10 mM | --- | --- | --- |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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