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Nicardipine hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Nicardipine hydrochloride图片
CAS NO:54527-84-3
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
500mg电议
1 g电议
5 g电议
10 g电议
50 g电议

产品名称
盐酸尼卡地平
YC-93
产品介绍
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。
生物活性

Nicardipine hydrochloride (YC-93) is acalcium channelblocker with anIC50of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure[1].

IC50& Target

IC50: 1 μM (cardiac calcium channels)[1]

体外研究
(In Vitro)

Nicardipine (0.1-10 μM; 24-48 h) reduces viability and proliferation of vascular smooth muscle cells (VSMCs) and inhibits their ability to migrate[2].

Cell Viability Assay[2]

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[1]

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
(In Vivo)

Nicardipine (0.3-10 mg/kg; p.o.) shows antihypertensive properties[3].
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[3].
LD50s of Nicardipine are 187 mg/kg (oral) and 15.5 mg/kg (intravenous) for male Wistar rats, respectively[3].
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[3].

Animal Model:In conscious normotensive rats (NR)[3]
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.
Clinical Trial
分子量

515.99

性状

Solid

Formula

C26H30ClN3O6

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, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and 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 mg5 mg10 mg
1 mM1.9380 mL9.6901 mL19.3802 mL
5 mM0.3876 mL1.9380 mL3.8760 mL
10 mM0.1938 mL0.9690 mL1.9380 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。