Nilvadipine (Synonyms:FK235; FR34235)
目录号 : KM3736 CAS No. : 75530-68-6 纯度 : 98%

Nilvadipine 是一种有效的钙离子通道 (calcium channel) 拮抗剂,IC50 为 0.1 nM。

规格 价格 是否有货 数量
10mg
In-stock
50mg
In-stock
100mg
In-stock
500mg
In-stock
1g 询价 In-stock
5g 询价 In-stock

Other Forms of Rapamycin:

KKL Med 的所有产品和服务仅用于科学研究,不能被用于人体,兽医,我们也不向个人提供产品和服务。
生物活性

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

体外研究

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. 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.

体内研究

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. 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.

分子式
C19H19N3O6
分子量
385.37
CAS号
75530-68-6
中文名称
尼伐地平
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (129.75 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

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

    此方案可获得 ≥ 3.33 mg/mL (8.64 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 33.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

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

    此方案可获得 3.33 mg/mL (8.64 mM) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 33.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

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

    此方案可获得 ≥ 3.33 mg/mL (8.64 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 33.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

临床试验
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
在线客服
咨询热线
400-881-9290
关注微信公众号