General description
A potent, specific, and orally active C5a receptor antagonist. Shown to inhibit the binding of 125I-rhC5a to human neutrophils with a Ki 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 Ki 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 Ki: 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
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- UPC:
- 51201829
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 234415-5MG
- CAS:
- 405098-33-1
- Temperature Control Device:
- Yes
