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Nisoldipine

MCE China：Nisoldipine

Brand：MedChemExpress (MCE)

Cat. No.HY-17402

CAS：63675-72-9

Synonyms：BAY-k 5552

Purity：99.36%

Storage：4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：Nisoldipine noncompetitively reduces the activity of human Paraoxonase 1, with an IC50 of 13.987 μM[3]. Nisoldipine (10-100 μM, 8-10 min) is about 30 times less selective for delayed-rectifier K+ channels than for L-type Ca2+ channels in fully polarised guinea-pig ventricular myocytes[4]. Nisoldipine also displays antioxidant potency with IC50 of 28.2 μM both before and after the addition of active oxygen[5]. Nisoldipine (1 μM, 90 s) largely prevents the elevation in [Ca2+]i caused by Lipopolysaccharide in Kupffer cells[6]. Nisoldipine (20 μM, 3 h pretreatment) exerts antiviral effect by interfering with the internalization of influenza A virus into A549 cells[7]. Nisoldipine (a cumulative manner from 1 to 10 and 100 nM at 5-min intervals) decreases elevated coronary perfusion pressure in NG-nitro-L-arginine (HY-12115)-perfused rat hearts[8].

In Vivo：Nisoldipine (10 ppm, intragastric feeding, 4 weeks) prevents alcoholic hepatitis caused by chronic intragastric ethanol exposure in the rat, possibly by inhibition of endotoxin-mediated Kupffer cell activation[1]. Nisoldipine (1000 ppm, diet, 12-14 weeks) prevents the development of hypertension and attenuates concomitant cardiac and aortic hypertrophy in spontaneously hypertensive rats[9]. Nisoldipine (1000 ppm, diet, 22 weeks) attenuates hypertension and protects the heart, reducing the incidence of microscopic scarring, reactive interstitial and perivascular fibrosis in spontaneously hypertensive rats[10]. Nisoldipine (20-40 mg/kg, intragastric gavage, daily, from day 2 to day 21) attenuates foot-shock-induced post-traumatic stress disorder and restores normal corticosterone levels in mice[11].

IC50 & Target：L-type calcium channel

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References：

[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.  [Content Brief]

[2]. Sidhu G, et al. Nisoldipine. 2024 Feb 28. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2025 Jan–.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[5]. Sugawara H, et al. Antioxidant effects of calcium antagonists on rat myocardial membrane lipid peroxidation. Hypertens Res. 1996 Dec;19(4):223-8.  [Content Brief]

[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.  [Content Brief]

[7]. Huang Y, et al. Nisoldipine Inhibits Influenza A Virus Infection by Interfering with Virus Internalization Process. Viruses. 2022 Dec 8;14(12):2738.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]