Nicardipine hydrochloride (Synonyms:盐酸尼卡地平; YC-93)
目录号 : KM3063 CAS No. : 54527-84-3 纯度 : 98%

Nicardipine hydrochloride (YC-93) 是一种钙通道 (calcium channel) 阻滞剂,可阻断心脏钙通道,IC50 为 1 μM。 Nicardipine hydrochloride 可用于研究慢性心绞痛以及控制血压。

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

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生物活性

Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.

体外研究

Nicardipine (0.1-10 μM; 24-48 h) reduces viability and proliferation of vascular smooth muscle cells (VSMCs) and inhibits their ability to migrate.

Cell Viability Assay

Cell Line: VSMCs were isolated from New Zealand rabbit aortic preparations
Concentration: 0.1 μM, 1 μM, 3 μM, 10 μM
Incubation Time: 24-48 hours
Result: Treatment reduced significantly cell viability and inhibited VSMCs proliferation in the presence of 10% FBS in a dose-dependent way, from 205.4±17.5% to 176.6±17%, 160.6±5.7%, 150.4±11.2%, 61.22±7.83% after 0.1 μM, 1 μM, 3 μM, 10 μM treatment, respectively.

Western Blot Analysis

Cell Line: BV-2 microglial cells
Concentration: 1, 3, 5, 10 μM
Incubation Time: 1 hours
Result: Reduced LPS/IFN-γ- and peptidoglycan-induced iNOS expression and COX-2 expression in a concentration-dependent manners.
体内研究

Nicardipine (0.3-10 mg/kg; p.o.) shows antihypertensive properties.
LD50s of Nicardipine are 643 mg/kg (oral) and 557 mg/kg (oral); 18.1 mg/kg (intravenous) 25.0 mg/kg (intravenous); 735 mg/kg (subcutaneous) and 683 mg/kg (subcutaneous); 171 mg/kg (intraperitoneally) and 155 mg/kg (intraperitoneally) for male and female Sprague-Dawley rats, respectively.
LD50s of Nicardipine are 187 mg/kg (oral) and 15.5 mg/kg (intravenous) for male Wistar rats, respectively.
LD50s of Nicardipine are 634 mg/kg (oral) and 650 mg/kg (oral); 20.7 mg/kg (intravenous) 19.9 mg/kg (intravenous); 540 mg/kg (subcutaneous) and 710 mg/kg (subcutaneous); 144 mg/kg (intraperitoneally) and 161 mg/kg (intraperitoneally) for male and female mice, respectively.

Animal Model: In conscious normotensive rats (NR)
Dosage: 0.3-10 mg/kg
Administration: P.o.
Result: Induced a dose-dependent hypotensive response (maximal decrease in mean blood pressure, supine position) without any postural hypotensive response.
分子式
C26H29N3O6.HCl
分子量
515.99
CAS号
54527-84-3
中文名称
盐酸尼卡地平
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 : ≥ 35 mg/mL (67.83 mM)

H2O : < 0.1 mg/mL (insoluble)

* "≥" 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 1.9380 mL 9.6901 mL 19.3802 mL
5 mM 0.3876 mL 1.9380 mL 3.8760 mL
10 mM 0.1938 mL 0.9690 mL 1.9380 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 (4.85 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.85 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.85 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.85 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

临床试验
科研文献
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
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