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.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| 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 |
| Dosages | 30 mg/kg |
| Administration | daily, s.c. |
| Molecular Weight | 580.61 |
| Formula | C32H24N2O7S |
| CAS Number | 2101765-81-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 2 mg/mL (Need ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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.
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