234415

C5a Receptor Antagonist, W-54011

The C5a Receptor Antagonist, W-54011, also referenced under CAS 405098-33-1, controls the biological activity of C5a Receptor.

• Synonyme(s) : C5a Receptor Antagonist, W-54011, N-((4-Dimethylaminophenyl)methyl)-N-(4-isopropylphenyl)-7-methoxy-1,2,3,4-tetrahydronaphthalen-1-carboxamide, HCl
• Formule empirique (notation de Hill): C₃₀H₃₆N₂O₂ · xHCl
• Numéro CAS: 405098-33-1
• Poids moléculaire : 456.62 (free base basis)
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic); protect from light
• Couleur: white
• Solubilité: DMSO: 50 mg/mL; methanol: 50 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• InChI: 1S/C30H36N2O2.ClH/c1-21(2)23-11-16-26(17-12-23)32(20-22-9-14-25(15-10-22)31(3)4)30(33)28-8-6-7-24-13-18-27(34-5)19-29(24)28;/h9-19,21,28H,6-8,20H2,1-5H3;1H
• Clé InChI: UKBJWRMNGCDKNL-UHFFFAOYSA-N

Description

Description générale

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).

Actions biochimiques/physiologiques

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

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable