DRI-C21045 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. DRI-C21045 (0.4-50 μM; 48 h) inhibits CD40L-induced MHC-II upregulation in THP-1 cells.
DRI-C21045 (30 mg/kg; s.c.; daily) prolongs graft survival in a murine allogeneic skin transplant model.
|Animal models||Full-thickness ear skins from BALB/c were transplanted onto the dorsal thorax of C57BL/6|
|Formulation||in 20% w/v hydroxypropyl-β-cyclodextrin (HPβCD) solution|
|Solubility (25°C)||DMSO 2 mg/mL (Need ultrasonic)|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Damir Bojadzic, et al. Curr Top Med Chem . Toward Small-Molecule Inhibition of Protein-Protein Interactions: General Aspects and Recent Progress in Targeting Costimulatory and Coinhibitory (Immune Checkpoint) Interactions
 Damir Bojadzic, et al. Curr Top Med Chem. Toward Small-Molecule Inhibition of Protein-Protein Interactions: General Aspects and Recent Progress in Targeting Costimulatory and Coinhibitory (Immune Checkpoint) Interactions
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