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234415

Sigma-Aldrich

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.

Sinónimos:

C5a Receptor Antagonist, W-54011, N-((4-Dimethylaminophenyl)methyl)-N-(4-isopropylphenyl)-7-methoxy-1,2,3,4-tetrahydronaphthalen-1-carboxamide, HCl

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About This Item

Fórmula empírica (notación de Hill):
C30H36N2O2 · xHCl
Número de CAS:
Peso molecular:
456.62 (free base basis)
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77

Nivel de calidad

Ensayo

≥95% (HPLC)

Formulario

solid

fabricante / nombre comercial

Calbiochem®

condiciones de almacenamiento

OK to freeze
desiccated (hygroscopic)
protect from light

color

white

solubilidad

DMSO: 50 mg/mL
methanol: 50 mg/mL

Condiciones de envío

ambient

temp. de almacenamiento

2-8°C

cadena SMILES

Cl.N(C)(C)c1ccc(cc1)CN(c4ccc(cc4)C(C)C)C(=O)C2CCCc3c2cc(cc3)OC

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

Clave InChI

UKBJWRMNGCDKNL-UHFFFAOYSA-N

Descripción general

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).

Acciones bioquímicas o fisiológicas

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

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

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

Información legal

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

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 1

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


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Tatjana Reif et al.
Cell reports. Medicine, 2(6), 100317-100317 (2021-07-02)
Polymorphonuclear neutrophils (PMNs), the most abundant white blood cells, are recruited rapidly to sites of infection to exert potent anti-microbial activity. Information regarding their role in infection with human immunodeficiency virus (HIV) is limited. Here we report that addition of

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