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Nilvadipine (Synonyms: CL 287,389, FK-235, FR34235, (±)-Nilvadipine, SKF 102362)

Catalog No.GC13698

Calcium channel inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

Nilvadipine Chemical Structure

Cas No.: 75530-68-6

Size Price Stock Qty
10mM (in 1mL DMSO)
$40.00
In stock
10mg
$34.00
In stock
50mg
$47.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Animal experiment:

Rat[4]In the present study, 3- to 5-week-old inbred RCS (rdy-/-) rats reared in cyclic light conditions (12 hours on-12 hours off) are used. Nilvadipine and Nifedipine are dissolved in a mixture of ethanol, polyethylene glycol 400, and distilled water (2:1:7) at a concentration of 0.1 mg/mL, diluted twice with physiological saline before use, and injected intraperitoneally (1.0 mL/kg) into anesthetized rats every day early in the morning for 2 weeks. In control rats, the same solution without Nilvadipine or Nifedipine (vehicle solution) is administered similarly. Nicardipine and Diltiazem are dissolved in PBS at 0.25 mg/mL and 1 mg/mL, respectively, and injected intraperitoneally (1 mL/kg), similarly to the other agonists. As a control, the same volume of a mixture of ethanol, polyethylene glycol 400, and distilled water (2:1:7) or PBS is administered. Before administration, the pH of all drug solutions is adjusted to approximately 7.4. The concentrations of these drugs administered to RCS rats are determined by their concentrations in oral administration to human patients with hypertension for 1 day in our clinical practice (Nilvadipine, 0.05-0.3 mg/kg; Nifedipine, 0.1-0.5 mg/kg; Nicardipine, 0.2-1 mg/kg; and Diltiazem, 0.3-3 mg/kg).

References:

[1]. Nomoto A, et al. Smooth muscle cell migration induced by inflammatory cell products and its inhibition by a potent calcium antagonist, Nilvadipine. Atherosclerosis. 1988 Aug;72(2-3):213-9.
[2]. Nomoto A, et al. Antiatherogenic activity of FR34235 (Nilvadipine), a new potent calcium antagonist. Effect on cuff-induced intimal thickening of rabbit carotid artery. Atherosclerosis. 1987 Apr;64(2-3):255-61.
[3]. Sugawara H, et al. Antioxidant effects of calcium antagonists on rat myocardial membrane lipid peroxidation. Hypertens Res. 1996 Dec;19(4):223-8.
[4]. Yamazaki H, et al. Preservation of retinal morphology and functions in royal college surgeons rat by Nilvadipine, a Ca(2+) antagonist. Invest Ophthalmol Vis Sci. 2002 Apr;43(4):919-26.

Background

Nilvadipine is a potent calcium channel antagonist, and the IC50 value is around 0.1 nM.

In an in vitro experiment on inhibition of migration of rat aortic smooth muscle cells, using Zymosan-activated air pouch exudate as a chemoattractant in modified Boyden chambers.The IC50 value is 0.033 nM for Nilvadipine (FR34235). Effects of Nilvadipine on proliferation of rat aortic smooth muscle cells and rabbit platelet aggregation is also examined. Nilvadipine should be useful for preventing and treating atherosclerosis. Inhibition of smooth muscle cell migration is thought to be its mechanism of antiatherogenic activity[2]. The antioxidant effect of calcium antagonist Nilvadipine is studied by means of rat myocardial membrane lipid peroxidation with a nonenzymatic active oxygen-generating system (DHF/FeC13-ADP) with IC50 of 25.1 μM. Nilvadipine shows antioxidant effects both before and after the addition of active oxygen, and reduces the dihydroxyfumarate (DHF) auto-oxidation rate, is chain-breaking and preventive antioxidants. Nicardipine, which shows an antioxidant effect only before exposure to active oxygen and reduced the DHF auto-oxidation rate, is mainly a preventive antioxidant[3].

The antiatherogenic activity of Nilvadipine (FR34235), a calcium antagonist, is examined in rabbits with carotid arteries sheathed with polyethylene cuffs, and compared with that of Nifedipine, Verapamil and Diltiazem. Nilvadipine is given intramuscularly in daily doses of 0.01-10 mg/kg for 3 weeks, starting on the day of cuff-placement. FR34235 dose-dependently inhibits the cuff-induced intimal thickening[2]. Nilvadipine affords significant protection against thinning of retinal layers in the RCS rat during retinal degeneration. Electron microscopy shows that marked irregularity in the photoreceptor OS in the untreated retina[4].

References:
[1]. Nomoto A, et al. Smooth muscle cell migration induced by inflammatory cell products and its inhibition by a potent calcium antagonist, Nilvadipine. Atherosclerosis. 1988 Aug;72(2-3):213-9.
[2]. Nomoto A, et al. Antiatherogenic activity of FR34235 (Nilvadipine), a new potent calcium antagonist. Effect on cuff-induced intimal thickening of rabbit carotid artery. Atherosclerosis. 1987 Apr;64(2-3):255-61.
[3]. Sugawara H, et al. Antioxidant effects of calcium antagonists on rat myocardial membrane lipid peroxidation. Hypertens Res. 1996 Dec;19(4):223-8.
[4]. Yamazaki H, et al. Preservation of retinal morphology and functions in royal college surgeons rat by Nilvadipine, a Ca(2+) antagonist. Invest Ophthalmol Vis Sci. 2002 Apr;43(4):919-26.

Chemical Properties

Cas No. 75530-68-6 SDF
Synonyms CL 287,389, FK-235, FR34235, (±)-Nilvadipine, SKF 102362
Chemical Name 3-O-methyl 5-O-propan-2-yl 2-cyano-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Canonical SMILES CC1=C(C(C(=C(N1)C#N)C(=O)OC)C2=CC(=CC=C2)[N+](=O)[O-])C(=O)OC(C)C
Formula C19H19N3O6 M.Wt 385.37
Solubility ≥ 12.4mg/mL in DMSO 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 2.5949 mL 12.9745 mL 25.9491 mL
5 mM 0.519 mL 2.5949 mL 5.1898 mL
10 mM 0.2595 mL 1.2975 mL 2.5949 mL
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