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67812-42-4

中文名稱 鹽酸去甲維拉帕米
英文名稱 NORVERAPAMIL HYDROCHLORIDE
CAS 67812-42-4
分子式 C26H37ClN2O4
分子量 477.04
MOL 文件 67812-42-4.mol
更新日期 2024/07/09 16:19:33
67812-42-4 結(jié)構(gòu)式 67812-42-4 結(jié)構(gòu)式

基本信息

中文別名
去甲維拉帕米
鹽酸去甲維拉帕米
去甲維拉帕米鹽酸鹽
鹽酸去甲維拉帕米(N-去甲 鹽酸維拉帕米)
英文別名
NORVERAPAMIL HCL
NORVERAPAMIL HYDROCHLORIDE
n-nor-(±)-verapamil hydrochloride
(±)-Norverapamill hydrochloride solution
(+/-)-VERAPAMIL, NOR-METHYL-, HYDROCHLORIDE
NorverapaMil HCl (N-DesMethyl VerapaMil HCl)
(+-)-VERAPAMIL HYDROCHLORIDE, NOR-METHYL (NORVERAPAMIL HYDROCH
a-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]propyl]-3,4-dimethoxy-a-(1-methylethyl)- benzeneacetonitril
a-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]propyl]-3,4-dimethoxy-a-(1-methylethyl)-benzeneacetonitrile
α-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]propyl]-3,4-dimethoxy-α-(1-methylethyl)- benzeneacetonitrile

物理化學(xué)性質(zhì)

熔點(diǎn)softens at 50°C, 155-160°C dec.
閃點(diǎn)9℃
儲(chǔ)存條件-20°C Freezer, Under Inert Atmosphere
溶解度H2O: >10 mg/mL
形態(tài)solid
顏色white
穩(wěn)定性吸濕性

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
危險(xiǎn)品運(yùn)輸編號(hào)UN 2811 6.1/PG 3
WGK Germany3

常見問題列表

生物活性
Norverapamil hydrochloride,是 Verapamil 的 N-去甲基代謝物,是一種鈣通道 (L-type calcium channel) 阻滯劑和 P-糖蛋白 (P-gp) 功能抑制劑。
靶點(diǎn)

Calcium channel blocker
P-glycoprotein (P-gp) inhibitor

體外研究

Norverapamil hydrochloride ((±)-Norverapamil hydrochloride) is similarly effective as verapamil at inhibiting isoniazid and rifampicin tolerance and killing of intracellular M. tuberculosis in the absence of other drugs. norverapamil, also inhibits macrophage-induced tolerance and achieves similar serum levels to verapamil.
Verapamil and its major metabolite norverapamil were identified to be both mechanism-based inhibitors and substrates of CYP3A and reported to have non-linear pharmacokinetics in clinic.

體內(nèi)研究

Norverapamil hydrochloride (9 mg/kg; p.o.), a major metabolite of verapamil, has terminal half-life, AUC and Cmax values of 9.4 hours, 260 ng?h/ml, and 41.6 ng/mL, respectively.

Animal Model: Male Sprague-Dawley rats
Dosage: 9 mg/kg (Pharmacokinetic Study)
Administration: Oral administration
Result: t 1/2 =9.4 hours; AUC=260 ng?h/mL; C max =41.6 ng/mL.
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