| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
Lercanidipine targets the L-type voltage-gated calcium channels (also known as dihydropyridine receptors) located primarily on vascular smooth muscle cells. It binds to the α1-subunit of the channel, specifically at the dihydropyridine binding site, and inhibits the influx of extracellular calcium ions into the cell. This blockade reduces the intracellular calcium concentration, which in turn prevents the calcium-calmodulin interaction required for the activation of myosin light-chain kinase. Consequently, vascular smooth muscle relaxation and vasodilation occur, reducing peripheral vascular resistance and lowering blood pressure.
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| ln Vitro |
In vitro, lercanidipine demonstrates high vascular selectivity and a pIC₅₀ of 7.74 (approximately 18 nM). Its vascular selectivity is higher than that of felodipine, another DHP-CCB. Lercanidipine displays only weak negative inotropic activity, meaning it has a minimal effect on the force of cardiac muscle contraction, which is a favorable property for an antihypertensive agent. This is due to its high lipophilicity, which leads to a high volume of distribution and a long duration of action at the vascular smooth muscle level.
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| ln Vivo |
In vivo, lercanidipine is an orally active antihypertensive agent with a long-lasting effect. Its high lipophilicity contributes to a prolonged duration of action, allowing for once-daily dosing. The compound is effective in reducing both systolic and diastolic blood pressure in hypertensive patients. Beyond its antihypertensive action, lercanidipine has demonstrated reno-protective and neuro-protective effects, as well as antioxidant, anti-inflammatory, and anti-apoptotic properties. These pleiotropic effects may provide additional cardiovascular benefits beyond blood pressure reduction.
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| Enzyme Assay |
Non-cell-based in vitro assays for lercanidipine are not typical, as its mechanism involves the inhibition of a membrane-bound ion channel. However, its binding affinity to the L-type calcium channel can be studied using radioligand binding assays with membrane preparations from cells expressing the channel. The receptor is incubated with a radiolabeled dihydropyridine ligand (e.g., [³H]-nitrendipine) and varying concentrations of lercanidipine. Its binding affinity (Ki) is determined by measuring the displacement of the radiolabeled ligand.
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| Cell Assay |
Cellular assays for lercanidipine are performed using vascular smooth muscle cells. Cells are treated with the compound, and intracellular calcium levels are measured using fluorescent dyes such as Fura-2. The compound's ability to inhibit depolarization-induced calcium influx is quantified. Its effects on vasoconstriction can be assessed using isolated blood vessel rings in tissue bath assays. These assays confirm the compound's functional activity as a calcium channel blocker.
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| Animal Protocol |
In vivo animal models for lercanidipine include spontaneously hypertensive rats (SHR) or other hypertensive models. The compound is administered orally, and its effect on blood pressure is measured over time using telemetry or the tail-cuff method. Its renal and neuroprotective effects can be assessed in models of renal injury or cerebral ischemia. These studies are crucial for establishing the in vivo antihypertensive efficacy and duration of action of the compound.
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| ADME/Pharmacokinetics |
Lercanidipine hydrochloride has a molecular weight of 648.21 g/mol and a molecular formula of C₃₆H₄₁N₃O₆·HCl. Its CAS number is 132866-11-6. The compound is a third-generation, lipophilic, brain-penetrant calcium channel blocker. It is supplied as a solid with a purity of ≥98%. Storage conditions: room temperature. The compound's high lipophilicity contributes to a prolonged duration of action and a high volume of distribution. Detailed pharmacokinetic parameters such as half-life and bioavailability are not extensively reported.
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| Toxicity/Toxicokinetics |
Lercanidipine hydrochloride has a well-established safety profile from its clinical use as an antihypertensive agent. Common side effects include peripheral edema, headache, and dizziness. The compound is for research use only in the context of this request and is not for human consumption. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
[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 |
Lercadipine hydrochloride is a diarylmethane.
Lercanidipine hydrochloride is a third-generation, lipophilic, vascular-selective, and orally active dihydropyridine calcium channel blocker. It is indicated for the treatment of hypertension. The compound has a pIC₅₀ of 7.74 and displays higher vascular selectivity than felodipine. It has a prolonged antihypertensive action as well as reno- and neuro-protective effects. Lercanidipine also shows antioxidant, anti-inflammatory, and anti-apoptotic properties. Its CAS number is 132866-11-6. |
| Molecular Formula |
C36H42CLN3O6
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|---|---|
| Molecular Weight |
648.19
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| Exact Mass |
647.276
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| CAS # |
132866-11-6
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| 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
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| PubChem CID |
157917
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| Appearance |
Light yellow to yellow solid powder
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| Boiling Point |
712.5ºC at 760mmHg
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| Melting Point |
175-177ºC
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| Flash Point |
384.7ºC
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| Vapour Pressure |
3.77E-20mmHg at 25°C
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| LogP |
8.132
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
46
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| Complexity |
1090
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| Defined Atom Stereocenter Count |
0
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| 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]
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| InChi Key |
WMFYOYKPJLRMJI-UHFFFAOYSA-N
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| 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
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| 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
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| Synonyms |
Corifeo Lerkamen Renovia Vasodip R 75 R-75 R75
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~77.14 mM)
H2O : < 0.1 mg/mL |
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| 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 |
*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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