C5a Receptor Antagonist, W-54011-CAS 405098-33-1-Calbiochem

C₃₀H₃₆N₂O₂ · xHCl

456.62 (free base basis)

A potent, specific, and orally active C5a receptor antagonist. Shown to inhibit the binding of ¹²⁵I-rhC5a to human neutrophils with a K_i of 2.2 nM, as well as C5a-induced intracellular Ca²⁺-mobilization, chemotaxis and reactive oxygen species (ROS) generation (IC₅₀ = 3.1 nM, 2.7 nM and 1.6 nM, respectively) with no agonist activity up to 10 µM. Shown to prevent C5a-induced neutrophenia in gerbils (100 µg/kg i.v. or 3-30 mg/kg orally).
A tetrahydronaphthalenyl carboxamide compound that acts as a potent, specific and orally active C5a receptor antagonist. Shown to inhibit the binding of ¹²⁵I-rhC5a to human neutrophils with a K_i of 2.2 nM, as well as C5a-induced intracellular Ca²⁺-mobilization, chemotaxis and reactive oxygen species (ROS) generation (IC₅₀ = 3.1 nM, 2.7 nM and 1.6 nM, respectively) with no agonist activity up to 10 µM. Shown to prevent C5a-induced neutrophenia in gerbils (100 µg/kg i.v. or 3-30 mg/kg orally).

Target IC₅₀: 3.1 nM, 2.7 nM and 1.6 nM against C5a-induced intracellular Ca2+-mobilization, chemotaxis and reactive oxygen species (ROS) generation, respectively
Primary Target
C5a Receptor
Product does not compete with ATP.
Target K_i: 2.2 nM against the binding of 125I-rhC5a to human neutrophils
Reversible: no
Cell permeable: no

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sumichika, H., et al. 2002. J. Biol. Chem.277, 49403.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
desiccated (hygroscopic)
protect from light

white

DMSO: 50 mg/mL
methanol: 50 mg/mL

ambient

2-8℃

1, 5 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 1