C5a Receptor Antagonist, W-54011 - CAS 405098-33-1 - Calbiochem (C15-1237-997)

General description

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).

Biochem/physiol Actions

Cell permeable: no

Primary Target
C5a Receptor

Product does not compete with ATP.

Reversible: no

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

Target K_i: 2.2 nM against the binding of 125I-rhC5a to human neutrophils

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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