Nisoldipine

Nisoldipine (BAY-k 5552; Sular) is an orally active and blood-brain barrier-penetrating dihydropyridine calcium antagonist, with greater vascular selectivity than other calcium channel antagonists. Nisoldipine inhibits calcium influx and blocks voltage-gated calcium channels. Nisoldipine dilates coronary and systemic arteries. Nisoldipine has antihypertensive and anti-anginal activity. Nisoldipine also displays neuroprotective and antiviral activity[1][2][7][11].

Product Specifications

CAS Number

[63675-72-9]

Product Name Alternative

BAY-k 5552

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Calcium Channel; Reactive Oxygen Species (ROS)

Type

Reference compound

Related Pathways

Immunology/Inflammation; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling; NF-κB

Applications

COVID-19-immunoregulation

Field of Research

Infection; Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Nisoldipine.html

Purity

99.56

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic)

Smiles

O=C(C1=C(C)NC(C)=C(C(OCC(C)C)=O)C1C2=CC=CC=C2[N+]([O-])=O)OC

Molecular Formula

C20H24N2O6

Molecular Weight

388.41

Precautions

H302, H315, H319, H335

References & Citations

[1]Hamilton SF, et al. Rapid-release and coat-core formulations of nisoldipine in treatment of hypertension, angina, and heart failure. Heart Dis. 1999 Nov-Dec;1 (5) :279-88.|[2]Sidhu G, et al. Nisoldipine. 2024 Feb 28. In: StatPearls [Internet]. Treasure Island (FL) : StatPearls Publishing; 2025 Jan–.|[3]Gökçe B, et al. Evaluation of in vitro effect, molecular docking, and molecular dynamics simulations of some dihydropyridine-class calcium channel blockers on human serum paraoxonase 1 (hPON1) enzyme activity. Biotechnol Appl Biochem. 2023 Oct;70 (5) :1707-1719. |[4]Missan S, et al. Block of cardiac delayed-rectifier and inward-rectifier K+ currents by nisoldipine. Br J Pharmacol. 2003 Nov;140 (5) :863-70.|[5]Sugawara H, et al. Antioxidant effects of calcium antagonists on rat myocardial membrane lipid peroxidation. Hypertens Res. 1996 Dec;19 (4) :223-8. |[6]Iimuro Y, et al. Nimodipine, a dihydropyridine-type calcium channel blocker, prevents alcoholic hepatitis caused by chronic intragastric ethanol exposure in the rat. Hepatology. 1996 Aug;24 (2) :391-7.|[7]Huang Y, et al. Nisoldipine Inhibits Influenza A Virus Infection by Interfering with Virus Internalization Process. Viruses. 2022 Dec 8;14 (12) :2738.|[8]Okada T, et al. Comparison of the effects of nifedipine and nisoldipine on coronary vasoconstriction in the Langendorff-perfused rat heart. J Cardiovasc Pharmacol. 2000 Jan;35 (1) :145-9.|[9] Godfraind T, et al. Effects of a chronic treatment by nisoldipine, a calcium antagonistic dihydropyridine, on arteries of spontaneously hypertensive rats. Circ Res. 1991 Mar;68 (3) :674-82. |[10]Campbell SE, et al. Cardiac structural remodelling after treatment of spontaneously hypertensive rats with nifedipine or nisoldipine. Cardiovasc Res. 1993 Jul;27 (7) :1350-8. |[11]Verma M, et al. Investigating the role of nisoldipine in foot-shock-induced post-traumatic stress disorder in mice. Fundam Clin Pharmacol. 2016 Apr;30 (2) :128-36.