| Size | Price | |
|---|---|---|
| 50mg | ||
| 100mg | ||
| 250mg |
| 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 (0.3–10 mg/kg) is an oral medication with antihypertensive effects [3]. Nicardipine's lethal dose (LD50) in male and female Sprague-Dawley rats is 643 mg/kg orally and 557 mg/kg orally; 18.1 mg/kg intravenously and 25.0 mg/kg intravenously; 735 mg/kg subcutaneously and 683 mg/kg kg subcutaneously; 171 mg/kg intraperitoneally and 155 mg/kg intraperitoneally [3]. Nicardipine's LD50 for male Wistar rats is 187 mg/kg when taken orally and 15.5 mg/kg when administered intravenously [3]. Nicardipine's lethal dose (LD50) for male and female mice is 634 mg/kg and 650 mg/kg, respectively; 20.7 mg/kg and 19.9 mg/kg, subcutaneous; 540 mg/kg and 710 mg/kg kg, subcutaneous; 144 mg/kg and 161 mg/kg, intraperitoneal [3].
|
| Cell Assay |
Cell Viability Assay[2]
Cell Types: VSMC isolated from New Zealand rabbit aorta preparation Tested Concentrations: 0.1 μM, 1 μM, 3 μM, 10 μM Incubation Duration: 24-48 hrs (hours) Experimental Results: Treatment Dramatically diminished cell viability and inhibited VSMC proliferation in the presence of 10% FBS was in a dose-dependent manner, ranging from 205.4±17.5% to 176.6±17%, 160.6±5.7%, 150.4±11.2%, and 61.22±7.83% after 0.1 μM, 1 μM, 3 μM, and 10 μM, respectively. treat. |
| Animal Protocol |
Animal/Disease Models: Conscious normotensive rat (NR)[3]
Doses: 0.3-10 mg/kg Route of Administration: Oral Experimental Results: Induced dose-dependent hypotensive response (maximum decrease in mean blood pressure, supine position) without any body positioning hypotensive reaction. |
| References |
[1]. Charnet P, et al. Electrophysiological analysis of the action of nifedipine and nicardipine on myocardial fibers. Fundam Clin Pharmacol. 1987;1(6):413-31.
[2]. R Stamatiou, et al. The dihydropyridine calcium antagonist nicardipine reduces aortic smooth muscle cell viability, proliferation and migration. Cardiovascular Research, 2018 Apr,114(1):S43. [3]. Sherrin H. Baky. Nic ardipine Hydrochloride. |
| Molecular Formula |
C26H29N3O6
|
|---|---|
| Molecular Weight |
479.525
|
| Exact Mass |
479.2056
|
| CAS # |
55985-32-5
|
| Related CAS # |
Nicardipine hydrochloride;54527-84-3;Nicardipine-d3 hydrochloride;1432061-50-1;(S)-Nicardipine;76093-36-2;(R)-Nicardipine;76093-35-1
|
| SMILES |
CC1=C(C(OC)=O)C(C2=CC([N+]([O-])=O)=CC=C2)C(C(OCCN(CC3=CC=CC=C3)C)=O)=C(C)N1
|
| Chemical Name |
3-(2-(benzyl(methyl)amino)ethyl) 5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
|
| Synonyms |
DaganFlusemideNicardipineCardeneAntagonil
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0854 mL | 10.4269 mL | 20.8538 mL | |
| 5 mM | 0.4171 mL | 2.0854 mL | 4.1708 mL | |
| 10 mM | 0.2085 mL | 1.0427 mL | 2.0854 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.
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