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Niguldipine (hydrochloride) (Synonyms: B 844-39,NSC 617553)

Catalog No.GC14919

α1A-adrenoceptor antagonist

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Niguldipine (hydrochloride) Chemical Structure

Cas No.: 119934-51-9

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5mg
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10mg
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25mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

Cas No. 119934-51-9 SDF
Synonyms B 844-39,NSC 617553
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
Formula C36H39N3O6 • HCl M.Wt 646.2
Solubility ≤10mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.5475 mL 7.7375 mL 15.4751 mL
5 mM 0.3095 mL 1.5475 mL 3.095 mL
10 mM 0.1548 mL 0.7738 mL 1.5475 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 11 reference(s) in Google Scholar.)

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