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W-54011

W-54011
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Purity:95.62%
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W-54011

Catalog No. T17250Cas No. 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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Pack SizePriceAvailabilityQuantity
1 mg$77In Stock
5 mg$129In Stock
10 mg$197In Stock
25 mg$353In Stock
50 mg$546In Stock
100 mg$787In Stock
1 mL x 10 mM (in DMSO)$168In Stock
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Product Introduction

Bioactivity
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 neutrophi
Targets&IC50
Ca2+ mobilization: 3.1 nM, ROS:1.6 nM(ki), C5aR:2.2 nM(Ki), Chemotaxis:2.7 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].
Chemical Properties
Molecular Weight493.08
FormulaC30H37ClN2O2
Cas No.405098-33-1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 28 mg/mL (56.79 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0281 mL10.1403 mL20.2807 mL101.4034 mL
5 mM0.4056 mL2.0281 mL4.0561 mL20.2807 mL
10 mM0.2028 mL1.0140 mL2.0281 mL10.1403 mL
20 mM0.1014 mL0.5070 mL1.0140 mL5.0702 mL
50 mM0.0406 mL0.2028 mL0.4056 mL2.0281 mL

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