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Purity: ≥98%
Nicardipine HCl (formerly YC-93, RS-69216; YC93; trade names Cardene, Dagan, Antagonil, Flusemide), the hydrochloride salt of nicardipine, is a dihydropyridine/DHP class of calcium-channel blocker (CCB) with anti-hypertensive activity. It has been approved for use in the treatment of high blood pressure, angina, chronic stable angina and Raynaud's phenomenon.
| Targets |
calcium channel (IC50 = 1 μM)
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| ln Vitro |
Vascular smooth muscle cells' (VSMC) viability, proliferation, and ability to migrate are all decreased by nicarcine (0.1–10 μM; 24-48 hours) [2].
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| ln Vivo |
Nicardipine has antihypertensive effects at doses of 0.3–10 mg/kg (po) [3]. The oral and subcutaneous LD50s of nicarcinine hydrochloride are 643 mg/kg and 557 mg/kg, respectively; the intravenous LD50s are 18.1 mg/kg and 25.0 mg/kg, while the subcutaneous LD50 is 683 mg/kg. kg (intraperitoneal); 171 mg/kg (subcutaneous); and 155 mg/kg (intraperitoneal) in Sprague-Dawley rats, the male and female, respectively [3]. In male Wistar rats, the LD50 of nicotricin hydrochloride is 187 mg/kg when administered orally, and 15.5 mg/kg when administered intravenously [3]. Nicardipine hydrochloride's LD50 values are as follows: 540 mg/kg (subcutaneous); 19.9 mg/kg (intravenous); 20.7 mg/kg (oral); and 710 mg/kg. kg (subcutaneous); for male and female mice, 144 mg/kg (intraperitoneal); and 161 mg/kg (intraperitoneal), respectively [3].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: VSMCs were isolated from New Zealand rabbit aortic preparations Tested Concentrations: 0.1 μM, 1 μM, 3 μM, 10 μM Incubation Duration: 24-48 hrs (hours) Experimental Results: Treatment decreased Dramatically 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 Types: BV-2 microglial cells Tested Concentrations: 1, 3, 5, 10 μM Incubation Duration: 1 hrs (hours) Experimental Results: decreased LPS/IFN-γ- and peptidoglycan-induced iNOS expression and COX -2 expression in a concentration-dependent manners. |
| Animal Protocol |
Animal/Disease Models: In conscious normotensive rats (NR)[3]
Doses: 0.3-10 mg/kg Route of Administration: Po Experimental Results: Induced a dose-dependent hypotensive response (maximal decrease in mean blood pressure, supine position) without any postural hypotensive response. |
| References |
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| Additional Infomation |
Nicardipine hydrochloride is a dihydropyridine. It has a role as a geroprotector.
Nicardipine Hydrochloride is the hydrochloride salt form of nicardipine, a synthetic derivative of nitrophenyl-pyridine and potent calcium channel blocker, Nicardipine (Nifedipine Family) blocks calcium ions from certain cell walls and inhibits contraction of coronary and peripheral arteries, resulting in lowered oxygen requirements for heart muscle and decreased arterial contraction and spasm. It is used clinically as a cerebral and coronary vasodilator. (NCI04) A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. See also: Nicardipine (has active moiety). |
| Molecular Formula |
C26H29N3O6.HCL
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| Molecular Weight |
515.99
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| Exact Mass |
515.182
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| Elemental Analysis |
C, 60.52; H, 5.86; Cl, 6.87; N, 8.14; O, 18.60
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| CAS # |
54527-84-3
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| Related CAS # |
Nicardipine-d3 hydrochloride;1432061-50-1;(S)-Nicardipine;76093-36-2;(R)-Nicardipine;76093-35-1;Nicardipine;55985-32-5
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| PubChem CID |
41114
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| Appearance |
Typically exists as light yellow to yellow solids at room temperature
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| Boiling Point |
603.4ºC at 760 mmHg
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| Melting Point |
176-1780C
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| Flash Point |
318.7ºC
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| LogP |
5.331
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
36
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| Complexity |
856
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=C(C)NC(C)=C(C(OCCN(C)CC2=CC=CC=C2)=O)C1C3=CC=CC([N+]([O-])=O)=C3)OC.[H]Cl
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| InChi Key |
AIKVCUNQWYTVTO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H29N3O6.ClH/c1-17-22(25(30)34-4)24(20-11-8-12-21(15-20)29(32)33)23(18(2)27-17)26(31)35-14-13-28(3)16-19-9-6-5-7-10-19;/h5-12,15,24,27H,13-14,16H2,1-4H3;1H
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| Chemical Name |
2-(Benzylmethylamino)ethyl methyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylatemonohydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04538534 | Completed | Drug: Nicardipine | Spasm Artery | Pr. Semir Nouira | November 1, 2020 | Phase 3 |
| NCT02271191 | Completed | Drug: Nicardipine | Spinal Stenosis | Yonsei University | May 2012 | Phase 4 |
| NCT06130527 | Not yet recruiting | Procedure: Nicardipine Procedure: Remifentanil |
Other Complications of Surgical and Medical Procedures |
Erol Karaaslan | November 30, 2023 | Not Applicable |
| NCT01810302 | Terminated Has Results | Drug: Nicardipine hydrochloride | Cerebral Vasospasm | University of Florida | August 2013 | Phase 2 |
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