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Niguldipine(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Niguldipine(hydrochloride)图片
CAS NO:119934-51-9
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
Cas No.119934-51-9
别名B 844-39,NSC 617553
化学名1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid, 3-[3-(4,4-diphenyl-1-piperidinyl)propyl] 5-methyl ester, monohydrochloride
Canonical SMILESO=C(C(C(C1=CC([N+]([O-])=O)=CC=C1)C(C(OC)=O)=C(C)N2)=C2C)OCCCN3CCC(C4=CC=CC=C4)(C5=CC=CC=C5)CC3.Cl
分子式C36H39N3O6o HCl
分子量646.2
溶解度≤10mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ki = 0.16 nM: α1A-adrenoceptor antagonist

IC50s = 0.4 μM: inhibits L-type Ca2+ channels

IC50s = 0.9 μM: suppresses T-type Ca2+ channels

Niguldipine is a less potent Ca2+ channel blocker and potent, selective α1A-adrenoceptor receptor antagonist. Ca2+ channels, expressed in the smooth muscles of the male reproductive tract, play a role in the physiological events involved in the seminal emission phase of ejaculation. It was demonstrated that α1-adrenoceptors, as members of superfamily of G protein-coupled receptors, are not a homogeneous population and have three distinct α1-adrenoceptor subtypes, involving α1A, α1B, and α1D.

In vitro: Niguldipine significantly increased the rate of long-lived protein degradation in human glioblastoma H4 cell, which indicated that niguldipine triggered autophagic degradation without inducing obvious cellular damage. Also, niguldipine blocked intracellular Ca2+ currents [1].

In vivo: Female Albino Swiss mice were administered intraperitoneally in a volume of 10 ml/kg niguldipine for 30 min. Niguldipine did not affect the electroconvulsive threshold in mice. Compared to the anticonvulsive activity of niguldipine against electroconvulsions, niguldipine remarkably impaired the protective action of both phenobarbital and carbamazepine [2].

References:
[1].  Zhang, L., Yu, J., Pan, H., Hu, P., Hao, Y., & Cai, W. et al. Small molecule regulators of autophagy identified by an image-based high-throughput screen. Proceedings of The National Academy of Sciences. 2007; 104(48): 19023-19028.
[2].  Borowicz, K., Gasior, M., Kleinrok, Z., & Czuczwar, S. Influence of isradipine, niguldipine and dantrolene on the anticonvulsive action of conventional antiepileptics in mice. European Journal of Pharmacology. 1997; 323(1): 45-51.