Identification | Back Directory | [Name]
N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE | [CAS]
405098-33-1 | [Synonyms]
W-54011 CS-2062 C5a Receptor Antagonist, W-54011 N-{[4-(diMethylaMino)phenyl]Methyl}-7-Methoxy-N-[4-(propan-2-yl)phenyl]-1,2,3,4-tetrahydronaphthalene-1-carboxaMide hydrochloride N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE | [Molecular Formula]
C30H37ClN2O2 | [MDL Number]
MFCD06659046 | [MOL File]
405098-33-1.mol | [Molecular Weight]
493.08 |
Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30 mg/mL; DMSO: 30 mg/mL; Ethanol: 3 mg/mL | [form ]
White powder solid. | [color ]
White to light yellow | [Stability:]
Hygroscopic |
Hazard Information | Back Directory | [Description]
W-54011 is an orally bioavailable, nonpeptide antagonist of complement component 5a receptor 1 (C5aR), also known as cluster of differentiation 88 (CD88).1 W-54011 inhibits 125I-rhC5a binding in neutrophils (Ki = 2.2 nM) and C5a-mediated intracellular Ca2+ mobilization (IC50 = 3.1 nM).1 W-54011 is selective and does not affect Ca2+ mobilization mediated by other G protein-coupled receptor (GPCR) ligands, N-Formyl-Met-Leu-Phe (fMLF; Item No. 21495), or IL-8 up to a concentration of 10 μM.1 It inhibits Ca2+ mobilization in neutrophils in humans, cynomolgus monkeys, and gerbils, but not in mice, rats, guinea pigs, rabbits, or dogs.1 At 10 nM, W-54011 also inhibits C5a-mediated migration and vessel formation of human microvascular endothelial cells (HMEC-1).2 | [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. |
| [storage]
Store at -20°C |
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Company Name: |
Musechem
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Tel: |
+1-800-259-7612 |
Website: |
www.musechem.com |
Company Name: |
Cckinase, Inc.
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Tel: |
+1 (732)236-3202 |
Website: |
www.cckinase.com |
Company Name: |
Wuhan Topule
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Tel: |
+86-02787215551 +86-19945035818 |
Website: |
http://www.topule.com/ |
Company Name: |
cjbscvictory
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Tel: |
13348960310 |
Website: |
https://www.weikeqi-biotech.com/ |
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