A selective C5aR antagonist (Ki = 2.2 nM); inhibitor of C5a-mediated Ca2+ mobilization in neutrophils (IC50 = 3.1 nM); does not affect Ca2+ mobilization in neutrophils mediated by fMLP or IL-8 up to a concentration of 10 μM

W-54011 – 25 mg

Brand:
Cayman
CAS:
405098-33-1
Storage:
-20
UN-No:
Non-Hazardous - /

W-54011 is an orally bioavailable, nonpeptide antagonist of complement component 5a receptor 1 (C5aR), also known as cluster of differentiation 88 (CD88).{34624} W-54011 inhibits 125I-rhC5a binding in neutrophils (Ki = 2.2 nM) and C5a-mediated intracellular Ca2+ mobilization (IC50 = 3.1 nM).{34624} W-54011 is selective and does not affect Ca2+ mobilization mediated by other G protein-coupled receptor (GPCR) ligands, N-Formyl-Met-Leu-Phe (fMLF; Item No. 21495), or IL-8 up to a concentration of 10 μM.{34624} It inhibits Ca2+ mobilization in neutrophils in humans, cynomolgus monkeys, and gerbils, but not in mice, rats, guinea pigs, rabbits, or dogs.{34624} At 10 nM, W-54011 also inhibits C5a-mediated migration and vessel formation of human microvascular endothelial cells (HMEC-1).{34625}  

 

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Description

A selective C5aR antagonist (Ki = 2.2 nM); inhibitor of C5a-mediated Ca2+ mobilization in neutrophils (IC50 = 3.1 nM); does not affect Ca2+ mobilization in neutrophils mediated by fMLP or IL-8 up to a concentration of 10 μM

Formal name: N-[[4-(dimethylamino)phenyl]methyl]-1,2,3,4-tetrahydro-7-methoxy-N-[4-(1-methylethyl)phenyl]-1-naphthalenecarboxamide, monohydrochloride

Synonyms: 

Molecular weight: 493.1

CAS: 405098-33-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area

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