ChemicalBook Product Catalog Biologics Biochemical Reagents Antagonist N-[[4-(Dimethylamino)phenyl]methyl]-1,2,3,4-tetrahydro-7-methoxy-N-[4-(1-methylethyl)phenyl]-1-naphthalenecarboxamide hydrochloride

N-[[4-(Dimethylamino)phenyl]methyl]-1,2,3,4-tetrahydro-7-methoxy-N-[4-(1-methylethyl)phenyl]-1-naphthalenecarboxamide hydrochloride

Product NameN-[[4-(Dimethylamino)phenyl]methyl]-1,2,3,4-tetrahydro-7-methoxy-N-[4-(1-methylethyl)phenyl]-1-naphthalenecarboxamide hydrochloride
CAS405098-33-1
MFC30H36N2O2.ClH
MW493.08
EINECS
MOL File405098-33-1.mol

Chemical Properties

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

Usage And Synthesis

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 (K_i = 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

References

[1] HIROSHI SUMICHIKA. Identification of a potent and orally active non-peptide C5a receptor antagonist.[J]. The Journal of Biological Chemistry, 2002, 277 51: 49403-49407. DOI: 10.1074/jbc.m209672200
[2] RYUJI KURIHARA. C5a promotes migration, proliferation, and vessel formation in endothelial cells.[J]. Inflammation Research, 2010, 59 8: 659-666. DOI: 10.1007/s00011-010-0178-4

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