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MedKoo Cat#: 318361 | Name: Nicardipine
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Nicardipine is a medication used to treat high blood pressure and angina. It belongs to the dihydropyridine class of calcium channel blockers. Nicardipine is a dihydropyridine calcium-channel blocking agent used for the treatment of vascular disorders such as chronic stable angina, hypertension, and Raynaud's phenomenon. It is available in oral and intravenous formulationss.

Chemical Structure

Nicardipine
Nicardipine
CAS#55985-32-5 (free base)

Theoretical Analysis

MedKoo Cat#: 318361

Name: Nicardipine

CAS#: 55985-32-5 (free base)

Chemical Formula: C26H29N3O6

Exact Mass: 479.2056

Molecular Weight: 479.53

Elemental Analysis: C, 65.12; H, 6.10; N, 8.76; O, 20.02

Price and Availability

Size Price Availability Quantity
250mg USD 230.00 2 Weeks
1g USD 380.00 2 Weeks
2g USD 610.00 2 Weeks
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Related CAS #
55985-32-5 (free base) 54527-84-3 (HCl) 156880-36-3 (phosphate)
Synonym
Nicardipine, Cardene, Antagonil, Dagan, Flusemide
IUPAC/Chemical Name
3-(2-(benzyl(methyl)amino)ethyl) 5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
InChi Key
ZBBHBTPTTSWHBA-UHFFFAOYSA-N
InChi Code
InChI=1S/C26H29N3O6/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
SMILES Code
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
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Nicardipine (YC-93 free base) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels.
In vitro activity:
This study has confirmed that nicardipine inhibits the breast cancer cells migration and colony formation. In addition, this study also revealed that nicardipine increases the Nrf2 and HO-1 expression. The inhibition of HO-1 abrogates nicardipine-reduced matrix metalloproteinase-9 expression. Reference: Front Pharmacol. 2021 Aug 13;12:710978. https://pubmed.ncbi.nlm.nih.gov/34483918/
In vivo activity:
This study examined whether nicardipine suppresses markers of microglial activation in vivo. The mean fluorescence intensity (M.F.I) reflecting intracellular IL-6 and TNF-α expression by microglia were reduced in the brains of mice that received LPS with nicardipine treatment (Fig. 6B and 6C). Microglial activation in the mouse brain was effectively attenuated by administration of nicardipine (Fig. 7). In addition, administration of nicardipine (50 mg/kg) alone did not affect microglia activation. Reference: PLoS One. 2014 Mar 12;9(3):e91167. https://pubmed.ncbi.nlm.nih.gov/24621589/
Solvent mg/mL mM comments
Solubility
DMSO 95.0 198.11
Ethanol 95.0 198.11
Water 30.0 62.56
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 479.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Chen YC, Chen JH, Tsai CF, Wu CT, Wu MH, Chang PC, Yeh WL. Nicardipine Inhibits Breast Cancer Migration via Nrf2/HO-1 Axis and Matrix Metalloproteinase-9 Regulation. Front Pharmacol. 2021 Aug 13;12:710978. doi: 10.3389/fphar.2021.710978. PMID: 34483918; PMCID: PMC8414136. 2. Kim DJ, Hwang MH, An TH, Jung KT. The relaxant effect of nicardipine on the isolated uterine smooth muscle of the pregnant rat. Anesth Pain Med (Seoul). 2019 Oct 31;14(4):429-433. doi: 10.17085/apm.2019.14.4.429. PMID: 33329773; PMCID: PMC7713808. 3. Ekins S, Puhl AC, Davidow A. Repurposing the Dihydropyridine Calcium Channel Inhibitor Nicardipine as a Nav1.8 Inhibitor In Vivo for Pitt Hopkins Syndrome. Pharm Res. 2020 Jun 11;37(7):127. doi: 10.1007/s11095-020-02853-5. PMID: 32529312; PMCID: PMC7702309. 4. Huang BR, Chang PC, Yeh WL, Lee CH, Tsai CF, Lin C, Lin HY, Liu YS, Wu CY, Ko PY, Huang SS, Hsu HC, Lu DY. Anti-neuroinflammatory effects of the calcium channel blocker nicardipine on microglial cells: implications for neuroprotection. PLoS One. 2014 Mar 12;9(3):e91167. doi: 10.1371/journal.pone.0091167. PMID: 24621589; PMCID: PMC3951295.
In vitro protocol:
1. Chen YC, Chen JH, Tsai CF, Wu CT, Wu MH, Chang PC, Yeh WL. Nicardipine Inhibits Breast Cancer Migration via Nrf2/HO-1 Axis and Matrix Metalloproteinase-9 Regulation. Front Pharmacol. 2021 Aug 13;12:710978. doi: 10.3389/fphar.2021.710978. PMID: 34483918; PMCID: PMC8414136. 2. Kim DJ, Hwang MH, An TH, Jung KT. The relaxant effect of nicardipine on the isolated uterine smooth muscle of the pregnant rat. Anesth Pain Med (Seoul). 2019 Oct 31;14(4):429-433. doi: 10.17085/apm.2019.14.4.429. PMID: 33329773; PMCID: PMC7713808.
In vivo protocol:
1. Ekins S, Puhl AC, Davidow A. Repurposing the Dihydropyridine Calcium Channel Inhibitor Nicardipine as a Nav1.8 Inhibitor In Vivo for Pitt Hopkins Syndrome. Pharm Res. 2020 Jun 11;37(7):127. doi: 10.1007/s11095-020-02853-5. PMID: 32529312; PMCID: PMC7702309. 2. Huang BR, Chang PC, Yeh WL, Lee CH, Tsai CF, Lin C, Lin HY, Liu YS, Wu CY, Ko PY, Huang SS, Hsu HC, Lu DY. Anti-neuroinflammatory effects of the calcium channel blocker nicardipine on microglial cells: implications for neuroprotection. PLoS One. 2014 Mar 12;9(3):e91167. doi: 10.1371/journal.pone.0091167. PMID: 24621589; PMCID: PMC3951295.
1: Samaniego EA, Dabus G, Generoso GM, Tari-Capone F, Fuentes K, Linfante I. Postpartum cerebral angiopathy treated with intra-arterial nicardipine and intravenous immunoglobulin. J Neurointerv Surg. 2013 May;5(3):e12. doi: 10.1136/neurintsurg-2011-010220. Epub 2012 Feb 19. Review. PubMed PMID: 22345147. 2: Peacock WF 4th, Hilleman DE, Levy PD, Rhoney DH, Varon J. A systematic review of nicardipine vs labetalol for the management of hypertensive crises. Am J Emerg Med. 2012 Jul;30(6):981-93. doi: 10.1016/j.ajem.2011.06.040. Epub 2011 Sep 9. Review. PubMed PMID: 21908132. 3: Lele A, Lyon T, Pollack A, Husmann K, Reeves A. Intra-arterial nicardipine for the treatment of cerebral vasospasm in postpartum cerebral angiopathy: a case study and review of literature. Int J Neurosci. 2011 Oct;121(10):537-42. doi: 10.3109/00207454.2011.598980. Epub 2011 Aug 4. Review. PubMed PMID: 21812738. 4: Habibzadeh MR, Thai H, Movahed MR. Prophylactic intragraft injection of nicardipine prior to saphenous vein graft percutaneous intervention for the prevention of no-reflow: a review and comparison to protection devices. J Invasive Cardiol. 2011 May;23(5):202-6. Review. PubMed PMID: 21562350. 5: Nij Bijvank SW, Duvekot JJ. Nicardipine for the treatment of severe hypertension in pregnancy: a review of the literature. Obstet Gynecol Surv. 2010 May;65(5):341-7. doi: 10.1097/OGX.0b013e3181e2c795. Review. PubMed PMID: 20591204. 6: Vadhera RB, Pacheco LD, Hankins GD. Acute antihypertensive therapy in pregnancy-induced hypertension: is nicardipine the answer? Am J Perinatol. 2009 Aug;26(7):495-9. doi: 10.1055/s-0029-1214251. Epub 2009 Apr 24. Review. PubMed PMID: 19396743. 7: Amenta F, Lanari A, Mignini F, Silvestrelli G, Traini E, Tomassoni D. Nicardipine use in cerebrovascular disease: a review of controlled clinical studies. J Neurol Sci. 2009 Aug 15;283(1-2):219-23. doi: 10.1016/j.jns.2009.02.335. Epub 2009 Mar 20. Review. PubMed PMID: 19303080. 8: Amenta F, Tomassoni D, Traini E, Mignini F, Veglio F. Nicardipine: a hypotensive dihydropyridine-type calcium antagonist with a peculiar cerebrovascular profile. Clin Exp Hypertens. 2008 Nov;30(8):808-26. doi: 10.1080/10641960802580190. Review. PubMed PMID: 19021030. 9: Hoh BL, Ogilvy CS. Endovascular treatment of cerebral vasospasm: transluminal balloon angioplasty, intra-arterial papaverine, and intra-arterial nicardipine. Neurosurg Clin N Am. 2005 Jul;16(3):501-16, vi. Review. PubMed PMID: 15990041. 10: Fischell TA, Maheshwari A. Current applications for nicardipine in invasive and interventional cardiology. J Invasive Cardiol. 2004 Aug;16(8):428-32. Review. PubMed PMID: 15282420. 11: Kouoh F, Gressier B, Dine T, Luyckx M, Brunet C, Ballester L, Cazin JC. Antioxidant effects and anti-elastase activity of the calcium antagonist nicardipine on activated human and rabbit neutrophils--a potential antiatherosclerotic property of calcium antagonists? Cardiovasc Drugs Ther. 2002 Dec;16(6):515-20. Review. PubMed PMID: 12766385. 12: Nicardipine. Dimens Crit Care Nurs. 2000 Nov-Dec;19(6):25. Review. PubMed PMID: 11998053. 13: Zannad F. Concomitant diseases in elderly hypertensives: the position of nicardipine. J Hypertens Suppl. 1996 Oct;14(3):S37-40. Review. PubMed PMID: 9120665. 14: Tobias JD. Nicardipine: applications in anesthesia practice. J Clin Anesth. 1995 Sep;7(6):525-33. Review. PubMed PMID: 8534474. 15: Sy J, Vitarelli A, Gheorghiade M. Nicardipine in heart failure: distinguishing its acute beneficial from its chronic effects. Minerva Cardioangiol. 1993 Nov;41(11):535-41. Review. PubMed PMID: 8127455. 16: Frampton JE, Faulds D. Nicardipine. A review of its pharmacology and therapeutic efficacy in older patients. Drugs Aging. 1993 Mar-Apr;3(2):165-87. Review. Erratum in: Drugs Aging 1996 Jul;9(1):36. PubMed PMID: 8477149. 17: Lambert CR. Combination therapy with nicardipine and beta-adrenergic blockade for angina pectoris. Clin Cardiol. 1992 Apr;15(4):231-4. Review. PubMed PMID: 1348670. 18: Chauveau D, Houillier P, Azizi M, Sassano P, Guyenne TT, Jeunemaître X, Plouin PF, Corvol P. [Use of intravenous nicardipine for the diagnosis of renovascular hypertension]. Arch Mal Coeur Vaiss. 1991 Aug;84(8):1171-5. Review. French. PubMed PMID: 1953265. 19: Whiting RL, Dow RJ, Graham DJ, Mroszczak EJ. An overview of the pharmacology and pharmacokinetics of nicardipine. Angiology. 1990 Nov;41(11 Pt 2):987-91. Review. PubMed PMID: 2248427. 20: Fifer MA, Aroney CN, Semigran MJ, Herrmann HC, Dec GW, Boucher CA. Techniques for assessing inotropic effects of drugs in patients with heart failure: application to the evaluation of nicardipine. Am Heart J. 1990 Feb;119(2 Pt 2):451-6. Review. PubMed PMID: 2405615.