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W54011

Chemical Structure : W54011

CAS No.: 405098-33-1

W54011 (W-54011)

Catalog No.: PC-38846Not For Human Use, Lab Use Only.

W-54011 (W54011) is a potent, selective, orally active and non-peptide C5a receptor antagonist, inhibits the binding of 125I-labeled C5a to human neutrophils with Ki of 2.2 nM.

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Biological Activity

W-54011 (W54011) is a potent, selective, orally active and non-peptide C5a receptor antagonist, inhibits the binding of 125I-labeled C5a to human neutrophils with Ki of 2.2 nM.
W-54011 also inhibited C5a-induced intracellular Ca2+ mobilization, chemotaxis, and generation of reactive super oxide species in human neutrophils with IC50 values of 3.1, 2.7, and 1.6 nM, respectively.
W-54011 did not show agonistic activity at up to 10 uM in C5a-induced intracellular Ca2+ mobilization assay with human neutrophils.
W-54011 effectively inhibited C5a-induced intracellular Ca2+ mobilization in neutrophils of cynomolgus monkeys and gerbils but not mice, rats, guinea pigs, rabbits, and dogs.
W-54011 (3-30 mg/kg, oral) inhibited C5a-induced neutropenia in a dose-dependent manner in gerbils.

Physicochemical Properties

M.Wt 493.088
Formula C30H37ClN2O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[(4-dimethylaminophenyl)methyl]-N-(4-isopropylphenyl)-7-methoxy-1,2,3,4-tetrahydronaphthalen-1- carboxamide hydrochloride

References

1. Xaria X Li, et al. Biochem Pharmacol. 2020 Oct;180:114156.

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