Cilnidipine - CAS:132203-70-4

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Cilnidipine (Synonyms:西尼地平; FRC-8653)

目录号 : KM11873 CAS No. : 132203-70-4 纯度 : 98%

Data Sheet 产品使用指南

Cilnidipine 是一种长效的第二代二氢吡啶类 Ca²⁺ 通道阻断剂，可有效作用于 L 和 N 型 Ca²⁺ 通道^[1]。具有抗高血压作用。

规格	价格	是否有货
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

Cilnidipine is a long-acting, second-generation dihydropyridine Ca-channel blocker on L and N-type Ca channel. Antihypertensive effects.

体外研究

Cilnidipine inhibits the L-type current with an IC₅₀ of 100 nM in neurons pretreated with omegaCgTx plus omegaAgTx.
The IC₅₀ for Cilnidipine in respect of the N-type current is 200 nM.
Cilnidipine dose- and time-dependently inhibits Ba currents in A7r5 cells with the IC₅₀ at 10 nM after 10 min.
Cilnidipine dose-dependently inhibits depolarization- and Ca-induced contractions of rat aortic rings, with an IC₅₀ of 10 nM at 10 min.
The viability of nPC12 cells show no significant change up to 150 μM Cilnidipine, but it decreases slightly in the cells treated with greater than 200 μM Cilnidipine.
Cilnidipine (100 μM, 2 hours) treatment increases the expression of p85aPI3K p-Akt, p-GSK-3β, and heat shock transcription factor (HSTF-1), and decreases levels of cytosolic cytochrome c, activated caspase 3, and cleaved PARP.

Cell Viability Assay

Cell Line:	Neuronally differentiated PC12 (nPC12) cells
Concentration:	0, 1, 5, 10, 25, 50, 100, 150, and 200 μM
Incubation Time:	Treated for 2 hours; cell viability was measured after 24 hours
Result:	Cell viability was not affected by low concentrations up to 150 μM, but it was slightly decreased at 200 μM.

Western Blot Analysis

Cell Line:	nPC12 cells
Concentration:	100 μM
Incubation Time:	2 hours
Result:	Increased the IRs of p58a PI3K, p-Akt, p-GSK-3β, and HSTF-1 and decreased the Immunoreactivities (IRs) of cytosolic cytochrome c, activated caspase 3 (17 kDa), and cleaved PARP (85 kDa).

体内研究

Cilnidipine has potent inhibitory actions on N-type as well as L-type voltage-dependent Ca-channel in rat dorsal root ganglion neurons.
Administration of Cilnidipine (10 mg/kg) and Nimodipine (10 mg/kg) significantly attenuates the immobilized stress-induced behavioral changes and restored memory deficits along with normalization of the corticosterone levels.
Cilnidipine and Nimodipine produce comparable beneficial effects in restoring immobilization stress subjected mice.
Oral administration of Cilnidipine (3 mg/kg) markedly lowers both systolic and diastolic blood pressure 1 hr after administration in 2K1C renal hypertensive dogs.

Animal Model:	Swiss albino mice weighing 25±5 g
Dosage:	5 and 10 mg/kg
Administration:	administered i.p. 30 min prior to immobilization stress
Result:	Cilnidipine (10 mg/kg, i.p.) and nimodipine (10 mg/kg, i.p.) 30 min prior to subjecting immobilization stress resulted in significant attenuation of immobilization stress-induced decrease in locomotor activity. Administration with Cilnidipine (5 mg/kg, i.p.) and Nimodipine (5 mg/kg, i.p.) did not show any significant effect on the stressed mice. Administration of Cilnidipine (10 mg/kg, i.p.) and Nimodipine (10 mg/kg, i.p.) in the non-stressed mice, and vehicle in the stressed mice did not modulate locomotor activity in a significant manner.

分子式

C₂₇H₂₈N₂O₇

分子量

492.52

CAS号

132203-70-4

中文名称

西尼地平

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (203.04 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	2.0304 mL	10.1519 mL	20.3037 mL
5 mM	0.4061 mL	2.0304 mL	4.0607 mL
10 mM	0.2030 mL	1.0152 mL	2.0304 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 (protect from light)。-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: ≥ 2.5 mg/mL (5.08 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.08 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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% corn oil
Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.08 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 25.0 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

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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The molarity calculator equation

The dilution calculator equation