W-54011 CAS#: 405098-33-1

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W-54011

用途生物活性靶点体外研究体内研究 用途与合成方法 MSDS W-54011价格(试剂级) 上下游产品信息

中文名称	W-54011
中文同义词	化合物 T17250;N-(4-(二甲氨基)苄基)-N-(4-异丙基苯基)-7-甲氧基-1,2,3,4-四氢萘-1-甲酰胺盐酸盐;化合物W-54011;W 54011,C5A受体拮抗剂
英文名称	N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE
英文同义词	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}-7-Methoxy-N-[4-(propan-2-yl)phenyl]-1,2,3,4-tetrahydronaphthalene-1-carboxaMide hydrochloride;W-54011;C5a Receptor Antagonist, W-54011;CS-2062;chemotaxis,inhibit,orally,W-54011,mobilization,anaphylatoxin,ROS,Reactive Oxygen Species,Ca2+,C5a,neutrophils,Inhibitor,Complement System,W54011,inflammatory,W 54011;N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE
CAS号	405098-33-1
分子式	C30H37ClN2O2
分子量	493.08
EINECS号
相关类别
Mol文件	405098-33-1.mol
结构式

W-54011 性质

W-54011 用途与合成方法

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.

安全信息

MSDS信息

W-54011 价格(试剂级)

W-54011 上下游产品信息