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Lemildipine (NB-818; NPK-1886; NPK 1886; NB 818; NB818; NPK1886) is a novel and potent calcium channel blocker (CCB) with potential anti-hypertensive activity.
| ln Vivo |
After the blockage is released, give gerbils intraperitoneal lemildipine (0.1-3 mg/kg) treatment. After four days of ischemia, they were perfused with 10% buffered formalin to fix them, and a microscope was used to measure the neuronal cell density (NCD, cells/mm) in the CA1 sector. The ischemia control group had a mean NCD of 43±10.8 cells/mm3, whereas lemildipine (3 mg/kg) dramatically increased DND to 143±24.2 cells/mm (P<0.01). Additionally, after 1–2–4 weeks of transient ischemia, Lemildipine (3 mg/kg) significantly reduced delayed neuronal death (DND). The average NCD in the Lemildipine group was 80±9.4 (P<0.01) and 43 were ±7.7 cells/mm, 92±13.7 (P<0.05) and 52±9.3 cells/mm, and 57±5.0 (P<0.01) and 43±12.4 cells/mm, respectively. Lemildipine (NB-818) was found to have a protective impact on DND in the hippocampus CA1 subregion following acute forebrain ischemia [1]. This effect persisted for a maximum of four weeks. Lemildipine (NPK-1886) at oral dosages of 3–30 mg/kg caused moderate decreases in blood pressure in normal Wistar rats (NWR). Remidipine and nifedipine have extremely comparable antihypertensive effects. On the other hand, lemildipine markedly lowered blood pressure in rats that were spontaneously hypertensive (SHR). A dose-dependent, statistically significant decrease in systolic blood pressure was observed upon oral administration of lemildipine at dosages of 3, 10, and 30 mg/kg. The greatest reduction was noticed one to three hours after medication. The dose-response curve at the maximal response during the course of the observation period (24 hours) was evaluated using the least squares approach in order to compare the antihypertensive efficacy of remidipine with nifedipine. Its potency was determined by calculating the dose that caused a 30% drop in blood pressure when compared to the control level (ED30). The ED30 values of remidipine and nifedipine are 10.2 mg/kg and 14.3 mg/kg, respectively; remidipine is 1.4 times more powerful than nifedipine [2].
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| References |
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| Additional Infomation |
Lemildipine is a dihydropyridine, an isopropyl ester and a methyl ester.
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| Molecular Formula |
C20H22CL2N2O6
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|---|---|
| Molecular Weight |
457.304
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| Exact Mass |
456.085
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| CAS # |
94739-29-4
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| PubChem CID |
65953
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| Appearance |
White to yellow solid powder
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| Density |
1.335±0.06 g/cm3 (20 °C, 760 mmHg)
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| Boiling Point |
585.6±50.0 °C (760 mmHg)
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| LogP |
4.457
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
30
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| Complexity |
764
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WTOVRSWDBLIFHU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H22Cl2N2O6/c1-9(2)30-19(26)16-13(8-29-20(23)27)24-10(3)14(18(25)28-4)15(16)11-6-5-7-12(21)17(11)22/h5-7,9,15,24H,8H2,1-4H3,(H2,23,27)
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| Chemical Name |
5-O-methyl 3-O-propan-2-yl 2-(carbamoyloxymethyl)-4-(2,3-dichlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
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| Synonyms |
NB-818NPK-1886NPK 1886NB 818 NB818 NPK1886
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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 |
| 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 : ~100 mg/mL (~218.67 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1867 mL | 10.9337 mL | 21.8675 mL | |
| 5 mM | 0.4373 mL | 2.1867 mL | 4.3735 mL | |
| 10 mM | 0.2187 mL | 1.0934 mL | 2.1867 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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