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W-54011

Cat. No. M9117
W-54011 Structure
Synonym:

W-54011 HCl

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1mg USD 200  USD200 Out of stock
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Quality Control & Documentation
Biological Activity

W-54011 is a potent, specific, and orally active CD88 (C5a receptor) antagonist, which inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca2+ mobilization, chemotaxis, and generation of reactive super oxide species in human neutrophils with IC50 alues of 3.1, 2.7, and 1.6 nM, respectively.

In vivo, in gerbils, oral administration of W-54011 (3-30 mg/kg) inhibits C5a-induced neutropenia in a dose-dependent manner. The present report is the first description of an orally active non-peptide C5a receptor antagonist that could contribute to the treatment of inflammatory diseases mediated by C5a.

Chemical Information
Molecular Weight 493.08
Formula C30H37ClN2O2
CAS Number 405098-33-1
Solubility (25°C) DMSO: ≥ 25 mg/mL
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] Sumichika H, et al. J Biol Chem. Identification of a potent and orally active non-peptide C5a receptor antagonist.

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