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MedKoo Cat#: 461087 | Name: Lercanidipine HCl
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Description:

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

Lercanidipine hydrochloride is a calcium channel blocker used in the treatment of hypertension.

Chemical Structure

Lercanidipine HCl
Lercanidipine HCl
CAS#132866-11-6 (HCl)

Theoretical Analysis

MedKoo Cat#: 461087

Name: Lercanidipine HCl

CAS#: 132866-11-6 (HCl)

Chemical Formula: C36H42ClN3O6

Exact Mass:

Molecular Weight: 648.20

Elemental Analysis: C, 66.71; H, 6.53; Cl, 5.47; N, 6.48; O, 14.81

Price and Availability

Size Price Availability Quantity
200mg USD 350.00 2 Weeks
1g USD 750.00 2 Weeks
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Related CAS #
132866-11-6 (HCl) 100427-26-7 (free base)
Synonym
Lercanidipine hydrochloride; Corifeo; Lerkamen; Renovia; Vasodip; R 75; R-75; R75;
IUPAC/Chemical Name
3-(1-((3,3-diphenylpropyl)(methyl)amino)-2-methylpropan-2-yl) 5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate hydrochloride
InChi Key
WMFYOYKPJLRMJI-UHFFFAOYSA-N
InChi Code
InChI=1S/C36H41N3O6.ClH/c1-24-31(34(40)44-6)33(28-18-13-19-29(22-28)39(42)43)32(25(2)37-24)35(41)45-36(3,4)23-38(5)21-20-30(26-14-9-7-10-15-26)27-16-11-8-12-17-27;/h7-19,22,30,33,37H,20-21,23H2,1-6H3;1H
SMILES Code
CC1=C(C(OC)=O)C(c2cc([N+]([O-])=O)ccc2)C(C(OC(C)(CN(CCC(c3ccccc3)c4ccccc4)C)C)=O)=C(C)N1.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
>3 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
2934.99.03.00
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Lercanidipine hydrochloride is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB).
In vitro activity:
Lercanidipine and amlodipine were found to show an enhanced effect with doxorubicin in inhibiting the growth of gastric cancer cells. While doxorubicin was identified to activate the pathways TGF-β and ERK/MAPK, lercanidipine was found to inhibit these pathways. Reference: Toxicol In Vitro. 2021 Aug;74:105152. https://pubmed.ncbi.nlm.nih.gov/33771646/
In vivo activity:
A total of 23 metabolites were altered significantly after cerebral ischaemic-reperfusion injury in MCAo control as compared to sham control rats. Lercanidipine significantly reduced the levels of valine, alanine, lactate, acetate and tyrosine, while N-acetylaspartate, glutamate, glutamine, aspartate, creatine/phosphocreatine, choline, glycerophosphorylcholine, taurine, myo-inositol and adenosine di-phosphate were elevated as compared to MCAo control. Reference: J Pharm Pharmacol. 2020 Jun;72(6):816-825. https://pubmed.ncbi.nlm.nih.gov/32163186/
Solvent mg/mL mM
Solubility
DMF 25.0 38.57
DMF:PBS (pH 7.2) (1:2) 0.3 0.46
DMSO 43.7 67.37
Ethanol 1.5 2.31
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 648.20 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. Panneerpandian P, Rao DB, Ganesan K. Calcium channel blockers lercanidipine and amlodipine inhibit YY1/ERK/TGF-β mediated transcription and sensitize the gastric cancer cells to doxorubicin. Toxicol In Vitro. 2021 Aug;74:105152. doi: 10.1016/j.tiv.2021.105152. Epub 2021 Mar 24. PMID: 33771646. 2. Wu JR, Liou SF, Lin SW, Chai CY, Dai ZK, Liang JC, Chen IJ, Yeh JL. Lercanidipine inhibits vascular smooth muscle cell proliferation and neointimal formation via reducing intracellular reactive oxygen species and inactivating Ras-ERK1/2 signaling. Pharmacol Res. 2009 Jan;59(1):48-56. doi: 10.1016/j.phrs.2008.09.015. Epub 2008 Oct 5. PMID: 18973813. 3. Gupta S, Sharma U, Jagannathan NR, Gupta YK. 1 H NMR metabolomic profiling elucidated attenuation of neurometabolic alterations by lercanidipine in MCAo model in rats. J Pharm Pharmacol. 2020 Jun;72(6):816-825. doi: 10.1111/jphp.13249. Epub 2020 Mar 12. PMID: 32163186. 4. Elbaz EM, Helmy HS, El-Sahar AE, Saad MA, Sayed RH. Lercanidipine boosts the efficacy of mesenchymal stem cell therapy in 3-NP-induced Huntington's disease model rats via modulation of the calcium/calcineurin/NFATc4 and Wnt/β-catenin signalling pathways. Neurochem Int. 2019 Dec;131:104548. doi: 10.1016/j.neuint.2019.104548. Epub 2019 Sep 17. PMID: 31539560.
In vitro protocol:
1. Panneerpandian P, Rao DB, Ganesan K. Calcium channel blockers lercanidipine and amlodipine inhibit YY1/ERK/TGF-β mediated transcription and sensitize the gastric cancer cells to doxorubicin. Toxicol In Vitro. 2021 Aug;74:105152. doi: 10.1016/j.tiv.2021.105152. Epub 2021 Mar 24. PMID: 33771646. 2. Wu JR, Liou SF, Lin SW, Chai CY, Dai ZK, Liang JC, Chen IJ, Yeh JL. Lercanidipine inhibits vascular smooth muscle cell proliferation and neointimal formation via reducing intracellular reactive oxygen species and inactivating Ras-ERK1/2 signaling. Pharmacol Res. 2009 Jan;59(1):48-56. doi: 10.1016/j.phrs.2008.09.015. Epub 2008 Oct 5. PMID: 18973813.
In vivo protocol:
1. Gupta S, Sharma U, Jagannathan NR, Gupta YK. 1 H NMR metabolomic profiling elucidated attenuation of neurometabolic alterations by lercanidipine in MCAo model in rats. J Pharm Pharmacol. 2020 Jun;72(6):816-825. doi: 10.1111/jphp.13249. Epub 2020 Mar 12. PMID: 32163186. 2. Elbaz EM, Helmy HS, El-Sahar AE, Saad MA, Sayed RH. Lercanidipine boosts the efficacy of mesenchymal stem cell therapy in 3-NP-induced Huntington's disease model rats via modulation of the calcium/calcineurin/NFATc4 and Wnt/β-catenin signalling pathways. Neurochem Int. 2019 Dec;131:104548. doi: 10.1016/j.neuint.2019.104548. Epub 2019 Sep 17. PMID: 31539560.
1: Wu Y, Xu M, Wang H, Xu X, Zhao S, Zhang M, Jin H, Yan J, Wang B, Gong J, Lu X, Peng J, Dai Q. Lercanidipine hydrochloride versus felodipine sustained-release for mild-to-moderate hypertension: a multi-center, randomized clinical trial. Curr Med Res Opin. 2015 Jan;31(1):171-6. doi: 10.1185/03007995.2014.960073. Epub 2014 Nov 26. PubMed PMID: 25425015. 2: Ranpise NS, Korabu SS, Ghodake VN. Second generation lipid nanoparticles (NLC) as an oral drug carrier for delivery of lercanidipine hydrochloride. Colloids Surf B Biointerfaces. 2014 Apr 1;116:81-7. doi: 10.1016/j.colsurfb.2013.12.012. Epub 2013 Dec 30. PubMed PMID: 24445002. 3: Vasigar P, Batmanabane M. Anti-inflammatoryactivity of calciumchannel blocker lercanidipine hydrochloride. J Pharmacol Pharmacother. 2013 Oct;4(4):238-42. doi: 10.4103/0976-500X.119707. PubMed PMID: 24250199; PubMed Central PMCID: PMC3825998. 4: Xu M, Wu Y, Wang H, Xu X, Zhao S, Zhang M, Jin H, Yan J, Wang B, Gong J, Lu X, Peng J, Dai Q. Effects of lercanidipine hydrochloride versus felodipine sustained-release on day-to-day home blood pressure variability. Curr Med Res Opin. 2016 Oct;32(sup2):43-52. PubMed PMID: 27779454. 5: Mehta S, Singh S, Chikhalia K. A fast, stability-indicating, and validated liquid chromatography method for the purity control of lercanidipine hydrochloride in tablet dosage form. Sci Pharm. 2014 Jan 16;82(2):327-40. doi: 10.3797/scipharm.1310-10. Print 2014 Apr-Jun. PubMed PMID: 24959405; PubMed Central PMCID: PMC4065126. 6: Shetty PK, Suthar NA, Menon J, Deshpande PB, Avadhani K, Kulkarni RV, Mutalik S. Transdermal delivery of lercanidipine hydrochloride: effect of chemical enhancers and ultrasound. Curr Drug Deliv. 2013 Aug;10(4):427-34. PubMed PMID: 23297866. 7: Derosa G, Bonaventura A, Romano D, Bianchi L, Fogari E, D'Angelo A, Maffioli P. Enalapril/lercanidipine combination on markers of cardiovascular risk: a randomized study. J Am Soc Hypertens. 2014 Jun;8(6):422-8. doi: 10.1016/j.jash.2014.03.329. Epub 2014 Apr 4. PubMed PMID: 24836352. 8: Derosa G, Bonaventura A, Romano D, Bianchi L, Fogari E, D'Angelo A, Maffioli P. Effects of enalapril/lercanidipine combination on some emerging biomarkers in cardiovascular risk stratification in hypertensive patients. J Clin Pharm Ther. 2014 Jun;39(3):277-85. doi: 10.1111/jcpt.12139. Epub 2014 Mar 17. PubMed PMID: 24635387. 9: Cao TS, Huynh VM, Tran VH. Effects of lercanidipine versus amlodipine in hypertensive patients with cerebral ischemic stroke. Curr Med Res Opin. 2015 Jan;31(1):163-70. doi: 10.1185/03007995.2014.964855. Epub 2014 Nov 26. PubMed PMID: 25425058. 10: Ha ES, Choo GH, Baek IH, Kim JS, Cho W, Jung YS, Jin SE, Hwang SJ, Kim MS. Dissolution and bioavailability of lercanidipine-hydroxypropylmethyl cellulose nanoparticles with surfactant. Int J Biol Macromol. 2015 Jan;72:218-22. doi: 10.1016/j.ijbiomac.2014.08.017. Epub 2014 Aug 23. PubMed PMID: 25159878. 11: Selvaraj N, Adhimoolam M, Perumal DK, Rajamohammed MA. Neuroprotective Effect of Lercanidipine- A Novel Calcium Channel Blocker in Albino Mice. J Clin Diagn Res. 2015 Nov;9(11):FF01-5. doi: 10.7860/JCDR/2015/14085.6801. Epub 2015 Nov 1. PubMed PMID: 26673531; PubMed Central PMCID: PMC4668433. 12: Yang Z. Efficacy and safety evaluation of perindopril-lercanidipine combined therapy in patients with mild essential hypertension. Curr Med Res Opin. 2015 Jan;31(1):183-6. doi: 10.1185/03007995.2014.960072. Epub 2014 Nov 26. PubMed PMID: 25424689. 13: Derosa G, Mugellini A, Querci F, Franzetti I, Pesce RM, D'Angelo A, Maffioli P. Barnidipine or Lercanidipine on Echocardiographic Parameters in Hypertensive, Type 2 Diabetics with Left Ventricular Hypertrophy: A Randomized Clinical Trial. Sci Rep. 2015 Aug 5;5:12603. doi: 10.1038/srep12603. PubMed PMID: 26243165; PubMed Central PMCID: PMC4525144. 14: Kaila HO, Ambasana MA, Thakkar RS, Saravaia HT, Shah AK. A Stability-indicating High Performance Liquid Chromatographic Assay for the Simultaneous Determination of Atenolol and Lercanidipine Hydrochloride in Tablets. Indian J Pharm Sci. 2011 Jul;73(4):376-80. doi: 10.4103/0250-474X.95612. PubMed PMID: 22707819; PubMed Central PMCID: PMC3374551. 15: Robles NR, Calvo C, Sobrino J, Espinel E, Esteban R, Mateos L, Macias JF. Lercanidipine valuable effect on urine protein losses: the RED LEVEL study. Curr Med Res Opin. 2016 Oct;32(sup2):29-34. PubMed PMID: 27779460. 16: Arnaout S; DUAL Investigators Study Group. Efficacy and safety of lercanidipine/enalapril fixed combination in Lebanon: a prospective observational study. Curr Med Res Opin. 2015 Jan;31(1):187-90. doi: 10.1185/03007995.2014.973938. Epub 2014 Nov 26. PubMed PMID: 25424779. 17: Minushkina LO, Iosava IK. [Lercanidipine in the treatment of arterial hypertension]. Kardiologiia. 2012;52(12):70-4. Review. Russian. PubMed PMID: 23237444. 18: Kaila HO, Ambasana MA, Thakkar RS, Saravaia HT, Shah AK. A Stability-indicating HPLC Method for Assay of Lercanidipine Hydrochloride in Tablets and for Determining Content Uniformity. Indian J Pharm Sci. 2010 May;72(3):381-4. doi: 10.4103/0250-474X.70490. PubMed PMID: 21188053; PubMed Central PMCID: PMC3003177. 19: Maldonado J, Pereira T, Tavares A. Efficacy and safety of a lercanidipine/enalapril fixed-dose combination in hypertensive patients in Portugal. Drugs R D. 2014 Jun;14(2):147-54. doi: 10.1007/s40268-014-0046-8. PubMed PMID: 24831818; PubMed Central PMCID: PMC4070459. 20: Gosteva EV, Vasil'eva LV. [Effect of Fixed Lercanidipine/Enalapril Combination on 24-Hour Blood Pressure Proffie in Elderly Patients With Arterial Hypertension]. Kardiologiia. 2015;55(2):32-6. Russian. PubMed PMID: 26164986.