Nicardipine hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

Nicardipine(YC-93) is a calcium channel blocker that has been widely used to control blood pressure in severe hypertension following events such as ischemic stroke, traumatic brain injury, and intracerebral hemorrhage.Hypertension Phase 3 Clinical(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.(In Vivo):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.

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.

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.

YC-93 Hydrochloride

GPCR/G Protein

Calcium Channel

AdrenergicReceptor|CalciumChannel|mAChR

Cardiovascular Disease

Hypertension

54527-84-3

515.9859

C26H30ClN3O6

>98% (HPLC)

DMSO: ≥ 35 mg/mL

CC1=C(C(C(=C(N1)C)C(=O)OCCN(C)Cc2ccccc2)c3cccc(c3)[N+](=O)[O-])C(=O)OC.Cl

3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 3-methyl 5-[2-[methyl(phenylmethyl)amino]ethyl] ester, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years