N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE
Uses- Product Name
- N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE
- CAS No.
- 405098-33-1
- Chemical Name
- N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE
- Synonyms
- W-54011;CS-2062;W-54011, 10 mM in DMSO;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;chemotaxis,inhibit,orally,W-54011,mobilization,anaphylatoxin,ROS,Reactive Oxygen Species,Ca2+,C5a,neutrophils,Inhibitor,Complement System,W54011,inflammatory,W 54011
- CBNumber
- CB4268080
- Molecular Formula
- C30H37ClN2O2
- Formula Weight
- 493.08
- MOL File
- 405098-33-1.mol
N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE Property
- 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
N-Bromosuccinimide Price
- Product number
- 234415
- Product name
- C5a Receptor Antagonist, W-54011 - CAS 405098-33-1 - Calbiochem
- Packaging
- 1mg
- Price
- $159
- Updated
- 2024/03/01
- Product number
- 234415
- Product name
- C5a Receptor Antagonist, W-54011 - CAS 405098-33-1 - Calbiochem
- Packaging
- 5mg
- Price
- $490
- Updated
- 2024/03/01
- Product number
- 21231
- Product name
- W-54011
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $40
- Updated
- 2024/03/01
- Product number
- 21231
- Product name
- W-54011
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $187
- Updated
- 2024/03/01
- Product number
- 21231
- Product name
- W-54011
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $315
- Updated
- 2024/03/01
N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE Chemical Properties,Usage,Production
Uses
W 54011 is a potent orally active non-peptide C5a receptor antagonist.
Description
W-54011 is an orally bioavailable, nonpeptide antagonist of complement component 5a receptor 1 (C5aR), also known as cluster of differentiation 88 (CD88). W-54011 inhibits 125I-rhC5a binding in neutrophils (Ki = 2.2 nM) and C5a-mediated intracellular Ca2+ mobilization (IC50 = 3.1 nM). 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; ), or IL-8 up to a concentration of 10 μM. It inhibits Ca2+ mobilization in neutrophils in humans, cynomolgus monkeys, and gerbils, but not in mice, rats, guinea pigs, rabbits, or dogs. At 10 nM, W-54011 also inhibits C5a-mediated migration and vessel formation of human microvascular endothelial cells (HMEC-1).
Uses
W 54011 is a potent orally active non-peptide C5a receptor antagonist.
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
N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE Preparation Products And Raw materials
Raw materials
Preparation Products
N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE Suppliers
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