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. |
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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. |
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| 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 | 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℃, 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。 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。 *以上所有助溶剂都可在本网站选购。
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