Art. -Nr.: HY-16992A

W-54011

6 Cited Publications

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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 K_i 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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Reinheit: 98.0%
CAS. Nr.: 405098-33-1
Formel: C₃₀H₃₇ClN₂O₂
Molecular Weight:493.08

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

W-54011 Chemical Structure

CAS. Nr.: 405098-33-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS. Nr. 405098-33-1
Appearance Solid
Molecular Weight 493.08
Formel C₃₀H₃₇ClN₂O₂
Color White to light yellow
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

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
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
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

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 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

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.

Protocol 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

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

W-54011

6 Cited Publications

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W-54011

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Autoimmune Disease Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) W-54011

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

W-54011

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Autoimmune Disease Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) W-54011

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

W-54011 Related Classifications

HY-16992A Related Classifications