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.

• Szinonimák: C5a Receptor Antagonist, W-54011, N-((4-Dimethylaminophenyl)methyl)-N-(4-isopropylphenyl)-7-methoxy-1,2,3,4-tetrahydronaphthalen-1-carboxamide, HCl
• Tapasztalati képlet (Hill-képlet): C₃₀H₃₆N₂O₂ · xHCl
• CAS-szám: 405098-33-1
• Molekulatömeg: 456.62 (free base basis)
• MDL-szám: MFCD26142284
• UNSPSC kód: 12352200
• NACRES: NA.77

Tulajdonságok

• Minőségi szint: 100
• Teszt: ≥95% (HPLC)
• Forma: solid
• gyártó/kereskedő neve: Calbiochem^®
• tárolási körülmény: OK to freeze; desiccated (hygroscopic); protect from light
• szín: white
• oldhatóság: DMSO: 50 mg/mL; methanol: 50 mg/mL
• kiszállítva: ambient
• tárolási hőmérséklet: 2-8°C
• SMILES string: 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
• Nemzetközi kémiai azonosító kulcs: UKBJWRMNGCDKNL-UHFFFAOYSA-N

Leírás

Általános leírás

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).

Biokémiai/fiziológiai hatások

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

Kiszerelés

Packaged under inert gas

Figyelmeztetés

Toxicity: Standard Handling (A)

Feloldás

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

Egyéb megjegyzések

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

Jogi információk

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

Biztonsági adatok

• Tárolási osztály kódja: 11 - Combustible Solids
• WGK: WGK 1
• Lobbanási pont (F): Not applicable
• Lobbanási pont (C): Not applicable