1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Calcium Channel
  3. Nilvadipine

Nilvadipine (Synonyms: FK235; FR34235)

Cat. No.: HY-14284 Purity: 99.96%
Handling Instructions

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

For research use only. We do not sell to patients.

Nilvadipine Chemical Structure

Nilvadipine Chemical Structure

CAS No. : 75530-68-6

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10 mM * 1  mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

IC50: 0.1 nM (Calcium channel)[1]

In Vitro

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].

In Vivo

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].

Clinical Trial
Molecular Weight

385.37

Formula

C₁₉H₁₉N₃O₆

CAS No.

75530-68-6

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (129.75 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5949 mL 12.9745 mL 25.9491 mL
5 mM 0.5190 mL 2.5949 mL 5.1898 mL
10 mM 0.2595 mL 1.2975 mL 2.5949 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.33 mg/mL (8.64 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 3.33 mg/mL (8.64 mM); Clear solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3.33 mg/mL (8.64 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[4]

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).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

NilvadipineFK235FR34235FK 235FK-235FR 34235FR-34235Calcium ChannelCa2+ channelsCa channelsInhibitorinhibitorinhibit

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Product name:
Nilvadipine
Cat. No.:
HY-14284
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