W-54011
Based on 6 publication(s) in Google Scholar
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.
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- Purity: 98.0%
- CAS No.: 405098-33-1
- 화학식: C30H37ClN2O2
- 분자량:493.08
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) W-54011
More- J Cell Mol Med. 2021 Jan;25(2):960-974. [Abstract]
- Med Microbiol Immunol. 2024 Sep 19;213(1):19. [Abstract]
- J Appl Oral Sci. 2023 Feb 3:31:e20220404. [Abstract]
- FEBS Open Bio. 2023 Mar;13(3):570-581. [Abstract]
- Eur J Oral Sci. 2025 Nov 26:e70054. [Abstract]
- Aging (Albany NY). 2021 Mar 10;13(6):8588-8598. [Abstract]
Biological Activity
Ki: 2.2 nM (C5a)sup>[1]
IC50: 3.1 nM (Ca2+ mobilization,), 2.7 nM (Chemotaxis), and 1.6 nM (ROS)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male mongolian gerbils (6-12 weeks) injected with rhC5a[1]
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Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:Oral administration; for 4 hours
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Result:Inhibited C5a-induced neutropenia in a dose-dependent manner.
Chemical Information
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CAS No. 405098-33-1
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Appearance Solid
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분자량 493.08
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화학식 C30H37ClN2O2
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Color White to light yellow
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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J Cell Mol Med
Complement C5 activation promotes type 2 diabetic kidney disease via activating STAT3 pathway and disrupting the gut-kidney axis. [Abstract]2021 Jan;25(2):960-974. PMID: 33280239 -
Med Microbiol Immunol
Exploration of compounds to inhibit the Panton-Valentine leukocidin of Staphylococcus aureus. [Abstract]2024 Sep 19;213(1):19. PMID: 39297970 -
J Appl Oral Sci
C5aR antagonist inhibits LPS-induced inflammation in human gingival fibroblasts via NF-κB and MAPK signaling pathways. [Abstract]2023 Feb 3:31:e20220404. PMID: 36753088 -
FEBS Open Bio
Determination of the optimal concentration and duration of C5aR antagonist application in an inflammatory model of human dental pulp cells. [Abstract]2023 Mar;13(3):570-581. PMID: 36732060 -
Eur J Oral Sci
Complement C5a receptor antagonist in the treatment of experimental periodontitis in mice. [Abstract]2025 Nov 26:e70054. PMID: 41299858 -
Aging (Albany NY)
Inhibition of complement C5a receptor protects lung cells and tissues against lipopolysaccharide-induced injury via blocking pyroptosis. [Abstract]2021 Mar 10;13(6):8588-8598. PMID: 33714207
용액&용해도
DMSO : ≥ 28 mg/mL (56.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0281 mL | 10.1403 mL | 20.2807 mL | 50.7017 mL |
| 5 mM | 0.4056 mL | 2.0281 mL | 4.0561 mL | 10.1403 mL | |
| 10 mM | 0.2028 mL | 1.0140 mL | 2.0281 mL | 5.0702 mL | |
| 15 mM | 0.1352 mL | 0.6760 mL | 1.3520 mL | 3.3801 mL | |
| 20 mM | 0.1014 mL | 0.5070 mL | 1.0140 mL | 2.5351 mL | |
| 25 mM | 0.0811 mL | 0.4056 mL | 0.8112 mL | 2.0281 mL | |
| 30 mM | 0.0676 mL | 0.3380 mL | 0.6760 mL | 1.6901 mL | |
| 40 mM | 0.0507 mL | 0.2535 mL | 0.5070 mL | 1.2675 mL | |
| 50 mM | 0.0406 mL | 0.2028 mL | 0.4056 mL | 1.0140 mL |
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