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DRI-C21045

Cat. No. M25496
DRI-C21045 Structure
Size Price Availability Quantity
10mg USD 260  USD260 In stock
50mg USD 660  USD660 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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.
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] 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

[2] 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

[3] Jinshui Chen, et al. J Med Chem. Small-Molecule Inhibitors of the CD40-CD40L Costimulatory Protein-Protein Interaction

[4] Jinshui Chen, et al. J Med Chem. Small-Molecule Inhibitors of the CD40-CD40L Costimulatory Protein-Protein Interaction

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