| CAS NO: | 119934-51-9 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 646.2 |
| Cas No. | 119934-51-9 |
| Formula | C36H39N3O6·HCl |
| Synonyms | B 844-39,NSC 617553 |
| Solubility | ≤10mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
| Chemical Name | 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 SMILES | O=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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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