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405098-33-1

中文名稱(chēng) W-54011
英文名稱(chēng) N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE
CAS 405098-33-1
分子式 C30H37ClN2O2
分子量 493.08
MOL 文件 405098-33-1.mol
更新日期 2026/05/21 12:26:49
405098-33-1 結(jié)構(gòu)式 405098-33-1 結(jié)構(gòu)式

基本信息

中文別名
化合物 T17250
化合物W-54011
N-(4-(二甲氨基)芐基)-N-(4-異丙基苯基)-7-甲氧基-1,2,3,4-四氫萘-1-甲酰胺鹽酸鹽
英文別名
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
所屬類(lèi)別
生物:拮抗劑

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMF: 30 mg/mL; DMSO: 30 mg/mL; Ethanol: 3 mg/mL
形態(tài)白色粉末狀固體。
顏色White to light yellow
穩(wěn)定性吸濕性

常見(jiàn)問(wèn)題列表

用途
W-54011是一種有效的口服非肽C5a受體拮抗劑。
生物活性
W-54011 是一種有效的,具有口服活性的非肽 C5a 受體拮抗劑。W-54011 抑制 125I 標(biāo)記的 C5a 與人嗜中性白細(xì)胞的結(jié)合,Ki 值為 2.2 nM。W-54011 還抑制 C5a 誘導(dǎo)的人嗜中性粒細(xì)胞的細(xì)胞內(nèi) Ca2+ 動(dòng)員,趨化性和 ROS 的生成,IC50 值分別為 3.1 nM、2.7 nM 和1.6 nM。
靶點(diǎn)

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

體外研究

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.

體內(nèi)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.

圖譜信息

W-54011價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2025/12/22HY-16992AW-54011
W-54011
405098-33-11mg690元
2025/12/22HY-16992AW-54011
W-54011
405098-33-15mg1400元
2025/12/22HY-16992AW-54011
W-54011
405098-33-110mM * 1mLin DMSO1519元
"405098-33-1" 相關(guān)產(chǎn)品信息
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