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MedKoo Cat#: 341127 | Name: Nicardipine hydrochloride
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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 formulations

Chemical Structure

Nicardipine hydrochloride
Nicardipine hydrochloride
CAS#54527-84-3 (HCl)

Theoretical Analysis

MedKoo Cat#: 341127

Name: Nicardipine hydrochloride

CAS#: 54527-84-3 (HCl)

Chemical Formula: C26H30ClN3O6

Exact Mass: 515.1823

Molecular Weight: 515.99

Elemental Analysis: C, 60.52; H, 5.86; Cl, 6.87; N, 8.14; O, 18.60

Price and Availability

Size Price Availability Quantity
1g USD 250.00 2 Weeks
5g USD 550.00 2 Weeks
10g USD 950.00 2 Weeks
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Related CAS #
55985-32-5 (free base) 54527-84-3 (HCl) 156880-36-3 (phosphate)
Synonym
Nicardipine hydrochloride ; YC-93; YC 93; YC93.
IUPAC/Chemical Name
2-(Benzylmethylamino)ethyl methyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylatemonohydrochloride
InChi Key
AIKVCUNQWYTVTO-UHFFFAOYSA-N
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
SMILES Code
CC1=C(C(C(=C(N1)C)C(=O)OCCN(C)Cc2ccccc2)c3cccc(c3)[N+](=O)[O-])C(=O)OC.Cl
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
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 hydrochloride (YC-93) is a calcium channel blocker with an IC50 of 1 μM.
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
DMF 20.0 38.76
DMSO 27.5 53.30
DMSO:PBS (pH 7.2) (1:2) 0.3 0.48
Ethanol 1.0 1.94
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 515.99 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: McKeever RG, Hamilton RJ. Calcium Channel Blockers. 2018 Feb 21. StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2018 Jan-. Available from http://www.ncbi.nlm.nih.gov/books/NBK482473/ PubMed PMID: 29494080. 2: Faro LRF, Alfonso M, Ferreira VM, Durán R. Role of voltage-gated calcium channels on striatal dopamine release induced by inorganic mercury in freely moving rats. Environ Toxicol Pharmacol. 2018 Feb 12;59:13-16. doi: 10.1016/j.etap.2018.02.005. [Epub ahead of print] PubMed PMID: 29482112. 3: Shimoyama Y, Umegaki O, Agui T, Kadono N, Minami T. Sudden onset of artery dissection in a 32-year-old woman with vascular Ehlers-Danlos syndrome due to psychological stress of her mother's death: a case series. JA Clin Rep. 2017;3(1):26. doi: 10.1186/s40981-017-0094-5. Epub 2017 May 8. PubMed PMID: 29457070; PubMed Central PMCID: PMC5804604. 4: Zhang P, Weeranoppanant N, Thomas DA, Tahara K, Stelzer T, Russell MG, O'Mahony M, Myerson AS, Lin H, Kelly LP, Jensen KF, Jamison TF, Dai C, Cui Y, Briggs N, Beingessner RL, Adamo A. Advanced Continuous Flow Platform for On-Demand Pharmaceutical Manufacturing. Chemistry. 2018 Feb 21;24(11):2776-2784. doi: 10.1002/chem.201706004. Epub 2018 Jan 31. PubMed PMID: 29385292. 5: Drumm BT, Rembetski BE, Cobine CA, Baker SA, Sergeant GP, Hollywood MA, Thornbury KD, Sanders KM. Ca(2+) signalling in mouse urethral smooth muscle in situ: role of Ca(2+) stores and Ca(2+) influx mechanisms. J Physiol. 2018 Jan 31. doi: 10.1113/JP275719. [Epub ahead of print] PubMed PMID: 29383731. 6: Kidd JM, Avery LM, Asempa TE, Nicolau DP, Kuti JL. Physical Compatibility of Meropenem and Vaborbactam With Select Intravenous Drugs During Simulated Y-site Administration. Clin Ther. 2018 Feb;40(2):261-269. doi: 10.1016/j.clinthera.2017.12.007. Epub 2017 Dec 28. PubMed PMID: 29290374. 7: Li J, Zhang YG, Luo LM, Dong X, Ding WH, Dang SY. Urotensin II promotes aldosterone expression in rat aortic adventitial fibroblasts. Mol Med Rep. 2018 Feb;17(2):2921-2928. doi: 10.3892/mmr.2017.8233. Epub 2017 Dec 8. PubMed PMID: 29257277; PubMed Central PMCID: PMC5783511. 8: Soomherun N, Kreua-Ongarjnukool N, Chumnanvej S, Thumsing S. Encapsulation of Nicardipine Hydrochloride and Release from Biodegradable Poly(D,L-lactic-co-glycolic acid) Microparticles by Double Emulsion Process: Effect of Emulsion Stability and Different Parameters on Drug Entrapment. Int J Biomater. 2017;2017:1743765. doi: 10.1155/2017/1743765. Epub 2017 Nov 8. PubMed PMID: 29250113; PubMed Central PMCID: PMC5698826. 9: Chudiwal VS, Shahi S, Chudiwal S. Development of sustained release gastro-retentive tablet formulation of nicardipine hydrochloride using quality by design (QbD) approach. Drug Dev Ind Pharm. 2018 May;44(5):787-799. doi: 10.1080/03639045.2017.1413111. Epub 2017 Dec 18. PubMed PMID: 29198152. 10: Lam M, Mast N, Pikuleva IA. Drugs and Scaffold That Inhibit Cytochrome P450 27A1 In Vitro and In Vivo. Mol Pharmacol. 2018 Feb;93(2):101-108. doi: 10.1124/mol.117.110742. Epub 2017 Nov 30. PubMed PMID: 29192124; PubMed Central PMCID: PMC5749491. 11: Orlov SN, Gusakova SV, Smaglii LV, Koltsova SV, Sidorenko SV. Vasoconstriction triggered by hydrogen sulfide: Evidence for Na(+),K(+),2Cl(-)cotransport and L-type Ca(2+) channel-mediated pathway. Biochem Biophys Rep. 2017 Nov 6;12:220-227. doi: 10.1016/j.bbrep.2017.09.010. eCollection 2017 Dec. PubMed PMID: 29159314; PubMed Central PMCID: PMC5683885. 12: Park ES, Kim DW, Kang SD. Endovascular Treatment of Symptomatic Vasospasm after Aneurysmal Subarachnoid Hemorrhage: A Three-year Experience. J Cerebrovasc Endovasc Neurosurg. 2017 Sep;19(3):155-161. doi: 10.7461/jcen.2017.19.3.155. Epub 2017 Sep 30. PubMed PMID: 29159148; PubMed Central PMCID: PMC5680078. 13: Smolyaninova LV, Koltsova SV, Sidorenko SV, Orlov SN. Augmented gene expression triggered by Na(+),K(+)-ATPase inhibition: Role of Ca(2+)(i)-mediated and -independent excitation-transcription coupling. Cell Calcium. 2017 Dec;68:5-13. doi: 10.1016/j.ceca.2017.10.002. Epub 2017 Oct 9. PubMed PMID: 29129208. 14: Hecht JP, Richards PG. Continuous-Infusion Labetalol vs Nicardipine for Hypertension Management in Stroke Patients. J Stroke Cerebrovasc Dis. 2018 Feb;27(2):460-465. doi: 10.1016/j.jstrokecerebrovasdis.2017.09.023. Epub 2017 Oct 31. PubMed PMID: 29092768. 15: Deguchi S, Mitsuya K, Nakasu Y, Hayashi N, Katagiri H, Murata H, Wasa J, Takahashi M, Endo M. Posterior reversible encephalopathy syndrome (PRES) induced by pazopanib, a multi-targeting tyrosine kinase inhibitor, in a patient with soft-tissue sarcoma: case report and review of the literature. Invest New Drugs. 2017 Oct 25. doi: 10.1007/s10637-017-0521-5. [Epub ahead of print] PubMed PMID: 29067537. 16: Ghattas MA, Bryce RA, Al Rawashdah S, Atatreh N, Zalloum WA. Comparative Molecular Dynamics Simulation of Aggregating and Non-Aggregating Inhibitor Solutions: Understanding the Molecular Basis of Promiscuity. ChemMedChem. 2017 Oct 23. doi: 10.1002/cmdc.201700654. [Epub ahead of print] PubMed PMID: 29058775. 17: Okuyama Y, Hirawa N, Fujita M, Fujiwara A, Ehara Y, Yatsu K, Sumida K, Kagimoto M, Katsumata M, Kobayashi Y, Saka S, Umemura S, Tamura K. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87. doi: 10.1038/hr.2017.92. Epub 2017 Oct 19. PubMed PMID: 29046519; PubMed Central PMCID: PMC5811637. 18: Akuzawa N, Kurabayashi M, Suzuki T, Yoshinari D, Kobayashi M, Tanahashi Y, Makita F, Saito R. Spontaneous isolated dissection of the superior mesenteric artery and aneurysm formation resulting from segmental arterial mediolysis: a case report. Diagn Pathol. 2017 Oct 16;12(1):74. doi: 10.1186/s13000-017-0664-x. PubMed PMID: 29037200; PubMed Central PMCID: PMC5644139. 19: Kamisah Y, Zuhair JSF, Juliana AH, Jaarin K. Parkia speciosa empty pod prevents hypertension and cardiac damage in rats given N(G)-nitro-l-arginine methyl ester. Biomed Pharmacother. 2017 Dec;96:291-298. doi: 10.1016/j.biopha.2017.09.095. Epub 2017 Oct 6. PubMed PMID: 28992471. 20: Stone ML, Kelly J, Mistry M, Buck M, Gangemi J, Vergales J. Use of Nicardipine After Cardiac Operations Is Safe in Children Regardless of Age. Ann Thorac Surg. 2018 Jan;105(1):181-185. doi: 10.1016/j.athoracsur.2017.05.035. Epub 2017 Oct 5. PubMed PMID: 28987396.