Nicardipine (YC-93 free base) 是一种钙通道 (calcium channel) 阻滞剂，可阻断心脏钙通道，IC50为 1 μM。Nicardipine 可用于研究慢性心绞痛以及控制血压。
| 生物活性 | Nicardipine (YC-93 free base) is acalcium channelblocker with anIC50of 1 μM for blocking cardiac calcium channels. Nicardipine 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. |
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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 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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