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67018-85-3

中文名稱 VERAPAMIL IMPURITY J
英文名稱 NORVERAPAMIL
CAS 67018-85-3
分子式 C26H36N2O4
分子量 440.58
MOL 文件 67018-85-3.mol
更新日期 2023/09/05 14:18:02
67018-85-3 結構式 67018-85-3 結構式

基本信息

中文別名
維拉帕米EP雜質J
化合物 T12244
鹽酸維拉帕米雜質J(EP) 標準品
英文別名
D591
NORVERAPAMIL
Norverapamil D6
Verapamil Impurity J
Verapamil EP Impurity J Monomer
(2RS)-2-(3,4-Dimethoxy-phenyl)-5-[[
2-(3,4-Dimethoxyphenyl)-2-isopropyl-5-(3,4-dimethoxyphenethylamino)valeronitrile
5-[(3,4-dimethoxyphenethyl)amino]-2-(3,4-dimethoxyphenyl)-2-isopropylvaleronitrile
α-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]propyl]-3,4-dimethoxy-α-isopropylbenzeneacetonitrile
Benzeneacetonitrile, α-[3-[[2-(3,4-dimethoxyphenyl)ethyl]amino]propyl]-3,4-dimethoxy-α-(1-methylethyl)-

物理化學性質

沸點586.1±50.0 °C(Predicted)
密度1.063±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)9.79±0.19(Predicted)
CAS 數(shù)據(jù)庫67018-85-3

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險
危險性描述H301

常見問題列表

生物活性
Norverapamil ((±)-Norverapamil),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

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

體外研究

Norverapamil ((±)-Norverapamil) 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.

體內研究

Norverapamil (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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