W-54011

用途生物活性靶点体外研究体内研究 W-54011 试剂级价格

W-54011

CAS号:405098-33-1
英文名:N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE
中文名:W-54011
CBNumber:CB4268080
分子式:C30H37ClN2O2
分子量:493.08
MOL File:405098-33-1.mol

W-54011化学性质

储存条件 :Store at -20°C
溶解度 :DMF: 30 mg/mL; DMSO: 30 mg/mL; Ethanol: 3 mg/mL
形态 :White powder solid.
颜色 :White to light yellow
稳定性 :Hygroscopic

W-54011性质、用途与生产工艺

用途 W-54011是一种有效的口服非肽C5a受体拮抗剂。
生物活性 W-54011 是一种有效的，具有口服活性的非肽 C5a 受体拮抗剂。W-54011 抑制 125I 标记的 C5a 与人嗜中性白细胞的结合，Ki 值为 2.2 nM。W-54011 还抑制 C5a 诱导的人嗜中性粒细胞的细胞内 Ca2+ 动员，趋化性和 ROS 的生成，IC50 值分别为 3.1 nM、2.7 nM 和1.6 nM。
靶点

Ki: 2.2 nM (C5a)sup>[1]
IC50: 3.1 nM (Ca ²⁺ mobilization,), 2.7 nM (Chemotaxis), and 1.6 nM (ROS)
体外研究

In C5a-induced intracellular Ca ²⁺ 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.

体内研究

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.
The species selectivity of W-54011 is examined in rhC5a-induced intracellular Ca ²⁺ mobilization of neutrophils in various species. The W-54011 is able to inhibit the response in cynomolgus monkeys and gerbils with IC ₅₀ values of 1.7 nM and 3.2 nM, respectively, but not in mice, rats, guinea pigs, rabbits, and dogs.

Animal Model:	Male mongolian gerbils (6-12 weeks) injected with rhC5a
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.