Nicardipine hydrochloride

SKU: orb1224730

Description

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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 54527-84-3
• MW: 515.9859
• Purity: >98% (HPLC)
• Formula: C₂₆H₃₀ClN₃O₆
• SMILES: CC1=C(C(C(=C(N1)C)C(=O)OCCN(C)Cc2ccccc2)c3cccc(c3)[N+](=O)[O-])C(=O)OC.Cl
• Target: Calcium Channel
• Solubility: DMSO: ≥ 35 mg/mL

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

YC-93 Hydrochloride

Quick Database Links

Gene Symbol

Calcium Channel