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W-54011

Catalog No. T17250 CAS 405098-33-1

W-54011 is a potent non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils (Ki = 2.2 nM). W-54011 inhibits C5a-induced intracellular Ca2+ mobilization, chemotaxis, and generation of ROS in human neutrophils (IC50s = 3.1 nM, 2.7 nM, and 1.6 nM, respectively).

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W-54011, CAS 405098-33-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 77.00
5 mg	In stock	$ 157.00
10 mg	In stock	$ 237.00
25 mg	In stock	$ 448.00
50 mg	In stock	$ 667.00
100 mg	In stock	$ 949.00
1 mL * 10 mM (in DMSO)	In stock	$ 168.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	W-54011 is a potent non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils (Ki = 2.2 nM). W-54011 inhibits C5a-induced intracellular Ca2+ mobilization, chemotaxis, and generation of ROS in human neutrophils (IC50s = 3.1 nM, 2.7 nM, and 1.6 nM, respectively).
Targets&IC50	Chemotaxis:2.7 nM(ki), Ca2+ mobilization: 3.1 nM, C5aR:2.2 nM(Ki), ROS:1.6 nM(ki)
In vitro	W-54011 does not show agonistic activity at up to 10 μM and shifts rightward the concentration-response curves to C5a without depressing the maximal responses, showing that W-54011 is a full antagonist. At concentrations up to 10 μM, W-54011 does not affect Ca2+ mobilization stimulated with sub-maximally effective concentrations of fMLP (1 nM), platelet-activating factor (0.3 nM), and IL-8 (0.1 nM)[1].
In vivo	W-54011 is able to inhibit the response in cynomolgus monkeys and gerbils (IC50 = 1.7 nM and 3.2 nM, respectively). In Male mongolian gerbils injected with rhC5a, W-54011 (3-30 mg/kg; oral; for 4 hours) inhibited C5a-induced neutropenia in a dose-dependent manner in gerbils. The species selectivity of W-54011 is examined in rhC5a-induced intracellular Ca2+ mobilization of neutrophils in various species [1].

Molecular Weight	493.08
Formula	C30H37ClN2O2
CAS No.	405098-33-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 28 mg/mL (56.79 mM)

References and Literature

1. Sumichika H, et al. Identification of a potent and orally active non-peptide C5a receptor antagonist. J Biol Chem. 2002 Dec 20;277(51):49403-49407.

Citations

1. Liu X, Wang W, Tan S, et al.C5a drives the inflammatory response with bacterial dose effect by binding to C5aR1 in zebrafish infected with Aeromonas hydrophila.Fish & Shellfish Immunology.2023: 108873.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Antioxidant Compound Library Metabolism Compound Library Bioactive Compounds Library Max Mitochondria-Targeted Compound Library Bioactive Compound Library Pyroptosis Compound Library Orally Active Compound Library Kinase Inhibitor Library NF-κB Signaling Compound Library

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Keywords

W-54011 405098-33-1 Immunology/Inflammation ROS Complement System W54011 chemotaxis inhibit orally W 54011 mobilization anaphylatoxin Reactive Oxygen Species Ca2+ C5a neutrophils Inhibitor inflammatory inhibitor

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