1. Immunology/Inflammation
    NF-κB
    Metabolic Enzyme/Protease
  2. Complement System
    Reactive Oxygen Species
  3. W-54011

W-54011 

Cat. No.: HY-16992A Purity: >98.0%
Handling Instructions

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

For research use only. We do not sell to patients.

W-54011 Chemical Structure

W-54011 Chemical Structure

CAS No. : 405098-33-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 208 In-stock
Estimated Time of Arrival: December 31
1 mg USD 96 In-stock
Estimated Time of Arrival: December 31
5 mg USD 192 In-stock
Estimated Time of Arrival: December 31
10 mg USD 288 In-stock
Estimated Time of Arrival: December 31
50 mg USD 900 In-stock
Estimated Time of Arrival: December 31
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200 mg   Get quote  

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Description

W-54011 is a potent and orally active non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca2+ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC50s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively[1].

IC50 & Target

Ki: 2.2 nM (C5a)sup>[1]
IC50: 3.1 nM (Ca2+ mobilization,), 2.7 nM (Chemotaxis), and 1.6 nM (ROS)[1]

In Vitro

In C5a-induced intracellular Ca2+ mobilization assay with human neutrophils, 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, indicating 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), plateletactivating factor (0.3 nM), and IL-8 (0.1 nM). This result demonstrates that W-54011 is highly specific for C5a receptor[1].

In Vivo

W-54011 (3-30 mg/kg; oral administration; for 4 hours; male mongolian gerbils) treatment inhibited C5a-induced neutropenia in a dose-dependent manner in gerbils[1].
The species selectivity of W-54011 is examined in rhC5a-induced intracellular Ca2+ mobilization of neutrophils in various species. The W-54011 is able to inhibit the response in cynomolgus monkeys and gerbils with IC50 values of 1.7 nM and 3.2 nM, respectively, but not in mice, rats, guinea pigs, rabbits, and dogs[1].

Animal Model: Male mongolian gerbils (6-12 weeks) injected with rhC5a[1]
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral administration; for 4 hours
Result: Inhibited C5a-induced neutropenia in a dose-dependent manner.
Molecular Weight

493.08

Formula

C₃₀H₃₇ClN₂O₂

CAS No.

405098-33-1

SMILES

O=C(C1CCCC2=C1C=C(OC)C=C2)N(CC3=CC=C(N(C)C)C=C3)C4=CC=C(C(C)C)C=C4.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 28 mg/mL (56.79 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0281 mL 10.1403 mL 20.2807 mL
5 mM 0.4056 mL 2.0281 mL 4.0561 mL
10 mM 0.2028 mL 1.0140 mL 2.0281 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: >98.0%

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Keywords:

W-54011W54011W 54011Complement SystemReactive Oxygen SpeciesC5aanaphylatoxinneutrophilsinflammatorymobilizationCa2+chemotaxisorallyROSInhibitorinhibitorinhibit

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W-54011
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