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Lercanidipine HCl (REC-15-237, Lercadip, Lerdip, Zanidip) is a 3rd generation and lipophilic CCB (calcium channel blocker) of the dihydropyridine class and a medication used to treat high blood pressure, with long lasting antihypertensive action and reno-protective effect. It works by relaxing and opening the blood vessels allowing the blood to circulate more freely around the body. This lowers the blood pressure and allows the heart to work more efficiently.
Physicochemical Properties
| Molecular Formula | C36H42CLN3O6 |
| Molecular Weight | 648.19 |
| Exact Mass | 647.276 |
| CAS # | 132866-11-6 |
| Related CAS # | Lercanidipine;100427-26-7;Lercanidipine-13C,d3 hydrochloride;1261397-71-0;Lercanidipine-13C,d3-1 hydrochloride;2747918-20-1;(R)-Lercanidipine;185197-70-0;(R)-Lercanidipine hydrochloride;187731-34-6;(S)-Lercanidipine hydrochloride;184866-29-3 |
| PubChem CID | 157917 |
| Appearance | Light yellow to yellow solid powder |
| Boiling Point | 712.5ºC at 760mmHg |
| Melting Point | 175-177ºC |
| Flash Point | 384.7ºC |
| Vapour Pressure | 3.77E-20mmHg at 25°C |
| LogP | 8.132 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 8 |
| Rotatable Bond Count | 13 |
| Heavy Atom Count | 46 |
| Complexity | 1090 |
| Defined Atom Stereocenter Count | 0 |
| SMILES | Cl[H].O(C(C1=C(C([H])([H])[H])N([H])C(C([H])([H])[H])=C(C(=O)OC([H])([H])[H])C1([H])C1C([H])=C([H])C([H])=C(C=1[H])[N+](=O)[O-])=O)C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])C([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C1C([H])=C([H])C([H])=C([H])C=1[H] |
| 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,20-21,23H2,1-6H31H |
| 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 |
| Synonyms | Corifeo Lerkamen Renovia Vasodip R 75 R-75 R75 |
| HS Tariff Code | 2934.99.9001 |
| 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, avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| References |
[1].Barrios, V., et al., Lercanidipine is an effective and well tolerated antihypertensive drug regardless the cardiovascular risk profile: The LAURA study. Int J Clin Pract, 2006. 60(11): p. 1364-70. [2].Burnier, M., M. Pruijm, and G. Wuerzner, Treatment of essential hypertension with calcium channel blockers: what is the place of lercanidipineExpert Opin Drug Metab Toxicol, 2009. 5(8): p. 981-7. [3].Grassi G, et, al. Lercanidipine in the Management of Hypertension: An Update. J Pharmacol Pharmacother. Oct-Dec 2017;8(4):155-165. [4]. Clinical efficacy of calcium channel blockers slow the third generation of lercanidipine in the treatment of patients with arterial hypertension and metabolic disorders (review). Georgian Med News. 2015 Feb;(239):51-6. Review. Russian. |
| Additional Infomation | Lercanidipine hydrochloride is a diarylmethane. |
Solubility Data
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~77.14 mM) H2O : < 0.1 mg/mL |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5428 mL | 7.7138 mL | 15.4276 mL | |
| 5 mM | 0.3086 mL | 1.5428 mL | 3.0855 mL | |
| 10 mM | 0.1543 mL | 0.7714 mL | 1.5428 mL |