产品
编 号:F620845
分子式:C32H24N2O7S
分子量:580.61
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5mg
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10mg
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50mg
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100mg
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生物活性:
DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC50 of 0.17 μM. DRI-C21045 shows concentration-dependent inhibition of the activation of NF-κB and B cell proliferation all induced by CD40L with IC50s of 17.1 μM and 4.5 μM, respectively.

体内研究:
DRI-C21045 (30 mg/kg; daily, s.c.; in 20% HPβCD) prolongs graft survival in a murine allogeneic skin transplant model.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).Animal Model:Full-thickness ear skins from BALB/c were transplanted onto the dorsal thorax of C57BL/6
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.

体外研究:
DRI-C21045 (3.2-100 μM; 18 h) concentration-dependently inhibits the CD40L-induced NF-κB activation in CD40 sensor cells.DRI-C21045 (0.6-50 μM; 48 h) blocks CD40L-induced functional activation of primary B cells.DRI-C21045 (0.4-50 μM; 48 h) inhibits CD40L-induced MHC-II upregulation in THP-1 cells.DRI-C21045 (2-100 μM; 48 h) inhibits CD40L-induced B cell proliferation.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.
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