W-54011

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的口服活性非肽 C5a 受体 (CD88;C5aR) 拮抗剂，Ki 为 2.2 nM。

A potent and orally active non-peptide C5a receptor (CD88;C5aR) antagonist with Ki of 2.2 nM; also inhibits C5a-induced intracellular Ca(2+) mobilization, chemotaxis, and generation of reactive super oxide species in human neutrophils with IC50 of 3.1, 2.7, and 1.6 nM, respectively; inhibits C5a-induced neutropenia in gerbils (3-30 mg/kg).

In C5a-induced intracellular Ca2+ mobilization assay with human neutrophils, W-54011 does not show agonistic activity at up to 10 μM and shifts rightward the concentration-response curves to C5a without depressing the maximal responses, indicating that W-54011 is a full antagonist. At concentrations up to 10 μM, W-54011 does not affect Ca2+ mobilization stimulated with sub-maximally effective concentrations of fMLP (1 nM), plateletactivating factor (0.3 nM), and IL-8 (0.1 nM). This result demonstrates that W-54011 is highly specific for C5a receptor.

W-54011 (3-30 mg/kg; oral administration; for 4 hours; male mongolian gerbils) treatment inhibited C5a-induced neutropenia in a dose-dependent manner in gerbils.The species selectivity of W-54011 is examined in rhC5a-induced intracellular Ca2+ mobilization of neutrophils in various species. The W-54011 is able to inhibit the response in cynomolgus monkeys and gerbils with IC50 values of 1.7 nM and 3.2 nM, respectively, but not in mice, rats, guinea pigs, rabbits, and dogs. Animal Model:Male mongolian gerbils (6-12 weeks) injected with rhC5a Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg Administration:Oral administration; for 4 hours Result:Inhibited C5a-induced neutropenia in a dose-dependent manner.

W54011 | W 54011 | W-54011

Immunology/Inflammation

Complement System

Complement System

Other Indications

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405098-33-1

493.08

C30H37ClN2O2

>98% (HPLC)

DMSO: ≥ 28 mg/mL

O=C(C1CCCC2=C1C=C(OC)C=C2)N(CC3=CC=C(N(C)C)C=C3)C4=CC=C(C(C)C)C=C4

1-Naphthalenecarboxamide, N-[[4-(dimethylamino)phenyl]methyl]-1,2,3,4-tetrahydro-7-methoxy-N-[4-(1-methylethyl)phenyl]-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years