1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel
  3. Lemildipine

Lemildipine  (Synonyms: NB-818; NPK-1886)

Cat. No.: HY-19663 Purity: 98.06%
COA Handling Instructions

Lemildipine is a new dihydropyridine calcium entry blocker.

For research use only. We do not sell to patients.

Lemildipine Chemical Structure

Lemildipine Chemical Structure

CAS No. : 94739-29-4

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mg USD 600 In-stock
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Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Lemildipine is a new dihydropyridine calcium entry blocker.

IC50 & Target

Calcium entry[1]

In Vivo

Gerbils are treated intraperitoneally with Lemildipine (0.1-3 mg/kg) just after release of the occlusion. Four days after the ischemia, they are fixed by perfusing 10% buffered-formalin, and the neuronal cell density (NCD, cell/mm) in the CA1 subfield is estimated under microscopy. The average NCD in the ischemic control group is 43±10.8 cells/mm, whereas Lemildipine (3 mg/kg) significantly ameliorates DND with an average NCD of 143±24.2 cells/mm (P<0.01). In addition, Lemildipine (3 mg/kg) significantly inhibits delayed neuronal death (DND) at 1, 2 and 4 weeks after transient ischemia: the average NCD of the Lemildipine and ischemic control groups are 80±9.4 (P<0.01) and 43±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. In this experiment, Lemildipine (NB-818) exhibits a protective effect on DND in the hippocampal CA1 subfield after transient forebrain ischemia, and its effect persisted for up to 4 weeks[1]. In normal Wistar rats (NWR), Lemildipine (NPK-1886) in doses of 3-30 mg/kg, p.o., produces a mild lowering of blood pressure. The depressor effect of Lemildipine is much the same as that of Nifedipine. In contrast, Lemildipine produces a significant decrease in the blood pressure of spontaneously hypertensive rats (SHR). Oral administration of Lemildipine in doses of 3, 10, 30 mg/kg produces a significant decrease in systolic blood pressure dose-dependently. The maximum decrease is observed 1-3 hr after administration. Comparing the hypotensive potency of Lemildipine and Nifedipine, their dose-response curves at the maximum response during the observation (for 24 hr) are analyzed by the least squares method, and the dose of 30% decrease in blood pressure from the control level (ED30) are used as a measure of their potency. Lemildipine is 1.4 times stronger than Nifedipine; the ED30 values of Lemildipine and Nifedipine are 10.2 mg/kg and 14.3 mg/kg, respectively[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

457.30

Formula

C20H22Cl2N2O6

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=C(COC(N)=O)NC(C)=C(C(OC)=O)C1C2=CC=CC(Cl)=C2Cl)OC(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (218.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Animal Administration
[1][2]

Gerbils[1]
Male Mongolian gerbils, weighing 50-80g, are used in this experiment. Lemildipine (3 mg/kg) or vehicle is administered intraperitoneally just after the recirculation. At 1, 2 or 4 weeks after ischemia, the animals are sacrificed, and the protective effect of Lemildipine (NB-818) is examined.
Mice and Rats[2]
Normal Wistar rats (NWR) and hypertensive model rats (spontaneously hypertensive rats (SHR), renal hypertensive rats (RHR) and DOCA-saline-induced hypertensive rats (DOC-Na-R)) of the male sex, weighing from 250 to 350 g, are used. Oral administration of Lemildipine in doses of 3, 10, 30 mg/kg for normal Wistar rats (NWR). Lethal dose of Lemildipine and Nifedipine is determined by the Litchfield-Wilcoxon method from the data of experiments using healthy mice and rats. Mice (male and female) weighing 20±2 g and male rats weighing from 150 to 220 g are used. These two kinds of animals are fed on solid food (Crea, CA-1) and water ad lib. The animal room temperature and humidity are controlled at 22±2°C and 55±5%, respecttively. No food except water is administered 24 hr before starting the experiments for oral administration of drugs.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1867 mL 10.9337 mL 21.8675 mL 54.6687 mL
5 mM 0.4373 mL 2.1867 mL 4.3735 mL 10.9337 mL
10 mM 0.2187 mL 1.0934 mL 2.1867 mL 5.4669 mL
15 mM 0.1458 mL 0.7289 mL 1.4578 mL 3.6446 mL
20 mM 0.1093 mL 0.5467 mL 1.0934 mL 2.7334 mL
25 mM 0.0875 mL 0.4373 mL 0.8747 mL 2.1867 mL
30 mM 0.0729 mL 0.3645 mL 0.7289 mL 1.8223 mL
40 mM 0.0547 mL 0.2733 mL 0.5467 mL 1.3667 mL
50 mM 0.0437 mL 0.2187 mL 0.4373 mL 1.0934 mL
60 mM 0.0364 mL 0.1822 mL 0.3645 mL 0.9111 mL
80 mM 0.0273 mL 0.1367 mL 0.2733 mL 0.6834 mL
100 mM 0.0219 mL 0.1093 mL 0.2187 mL 0.5467 mL
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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