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W54011 (W-54011) is a novel, high affinity and orally bioactive non-peptide C5a receptor (CD88) antagonist (Ki = 2.2 nM) with the potential to be used for the treatment of inflammatory diseases mediated by C5a. W54011 inhibits C5a-induced generation of reactive superoxide species, chemotaxis and intracellular Ca2+ mobilization in human neutrophils (IC50 are 1.6, 2.7 and 3.1 nM, respectively).
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| ln Vitro |
W-54011 is a complete antagonist since it moves the concentration-response curves to the right of C5a without lowering the peak responses in the C5a-induced intracellular Ca2+ mobilization experiment with human neutrophils and does not exhibit agonistic activity at concentrations as high as 10 μM. W-54011 has no effect at concentrations up to 10 μM on Ca2+ mobilization triggered with sub-maximally efficacious quantities of IL-8 (0.1 nM), fMLP (1 nM), and platelet-activating factor (0.3 nM). W-54011 is extremely selective for the C5a receptor, as this data shows[1].
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| ln Vivo |
In male mongolian gerbils, oral administration of W-54011 (3-30 mg/kg) for four hours reduced C5a-induced neutropenia in a dose-dependent manner[1]. In the context of rhC5a-induced intracellular Ca2+ mobilization of neutrophils in different species, the species selectivity of W-54011 is investigated. With IC50 values of 1.7 nM and 3.2 nM, respectively, the W-54011 can block the reaction in cynomolgus monkeys and gerbils, but not in mice, rats, guinea pigs, rabbits, or dogs[1].
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| Animal Protocol |
Animal/Disease Models: Male mongolian gerbils (6-12 weeks) injected with rhC5a[1]
Doses: 3 mg/kg, 10 mg/kg, 30 mg/kg Route of Administration: Oral administration; for 4 hrs (hours) Experimental Results: Inhibited C5a-induced neutropenia in a dose-dependent manner. |
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| References | ||
| Additional Infomation |
W54011 is potent, specific and orally active C5a receptor antagonist It has a role as an anti-inflammatory agent and a C5a receptor antagonist.
See also: W54011 (annotation moved to). |
| Molecular Formula |
C30H36N2O2
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|---|---|
| Molecular Weight |
493.07998
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| Exact Mass |
492.254
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| CAS # |
405098-33-1
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| PubChem CID |
5311121
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| Appearance |
White to light yellow solid powder
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| Boiling Point |
619ºC at 760 mmHg
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| Flash Point |
328.2ºC
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| LogP |
7.467
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
35
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| Complexity |
634
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DVYASSBBADJRAS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H36N2O2/c1-21(2)23-11-16-26(17-12-23)32(20-22-9-14-25(15-10-22)31(3)4)30(33)28-8-6-7-24-13-18-27(34-5)19-29(24)28/h9-19,21,28H,6-8,20H2,1-5H3
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| Chemical Name |
N-[(4-dimethylaminophenyl)methyl]-7-methoxy-N-(4-propan-2-ylphenyl)-1,2,3,4-tetrahydronaphthalene-1-carboxamide
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| Synonyms |
W-54011 W 54011 W54011
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 28 mg/mL (~56.79 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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