W-54011

SKU: orb1307610

Description

W-54011 is a potent, non-peptide antagonist of the C5a receptor (C5aR1). It effectively blocks C5a binding (Ki = 2.2 nM) and inhibits downstream functional responses in human neutrophils, including calcium mobilization, chemotaxis, and ROS generation. This compound is a valuable research tool for studying complement-mediated inflammation in both in vitro and in vivo models.

Research Area

Immunology & Inflammation, Metabolism Research, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	405098-33-1
MW	493.08
Purity	96.80% (May vary between batches)
Formula	C₃₀H₃₇ClN₂O₂
SMILES	Cl.COc1ccc2CCCC(C(=O)N(Cc3ccc(cc3)N(C)C)c3ccc(cc3)C(C)C)c2c1
Target	ROS,Complement System,Reactive Oxygen Species
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.06 mM);DMSO:28 mg/mL (56.79 mM)

Bioactivity

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Target IC50	ROS:1.6 nM(ki)\|C5aR:2.2 nM(Ki)\|Chemotaxis:2.7 nM(ki)\|Ca2+ mobilization: 3.1 nM
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 . Read more...
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). Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Ca2+, C5a, Ca2+ mobilization,, anaphylatoxin, Complement System, ComplementSystem, complement 5a receptor (C5aR), chemotaxis, Chemotaxis, orally, mobilization, neutrophils, inhibit, inflammatory, Inhibitor, W 54011, W54011, W-54011, Reactive Oxygen Species, ROS

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Compound Identifiers

PubChem CID

5311121 ↗

Key Properties

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No computed properties available.

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W-54011 (orb1307610)

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W-54011

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Compound Identifiers

Key Properties

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Protocol Information

W-54011 (orb1307610)

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