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

Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer.

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

Amlodipine Chemical Structure

Amlodipine Chemical Structure

CAS No. : 88150-42-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
500 mg USD 55 In-stock
1 g USD 92 In-stock
5 g USD 290 In-stock
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Amlodipine:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer[1][2][3].

IC50 & Target[1]

L-type calcium channel

 

Cellular Effect
Cell Line Type Value Description References
LLC-MK2 IC50
70.82 μM
Compound: Amlodipine
Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
[PMID: 20934347]
LLC-MK2 IC50
8.07 μM
Compound: Amlodipine
Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
[PMID: 20934347]
Oocyte IC50
1.2 μM
Compound: Amlodipine
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
[PMID: 22761000]
Oocyte IC50
4.2 μM
Compound: Amlodipine
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
[PMID: 22761000]
Ventricular myocyte IC50
0.57 μM
Compound: Amlodipine
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
[PMID: 22761000]
In Vitro

Amlodipine (20-40 μM; 48 h) reduces BrdU incorporation to 68.6% and 26.3% at concentrations of 20 and 30 μM in A431 cells, respectively[3].
Amlodipine (30 μM; pretreated for 1 h) significantly attenuates the uridine 5′-triphosphate (UTP)-induced increases of [Ca2+]i in A431 cells[3].
Amlodipine (30 μM) inhibits the store-operated Ca2+influx evoked by Thapsigargin in Fluo-3-loaded cells[3].

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

In Vivo

Amlodipine (5 mg/kg/day; s.c. for 2 weeks) significantly decreases systolic blood pressure (SBP) in VSMC ATP2B1 KO mice[4].
Amlodipine (10 mg/kg; i.p. once daily for 20 days) causes a significant retardation of tumor growth and prolongs the survival of A431 tumor-bearing mice[3].

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

Animal Model: ATP2B1loxP/loxP mice[4]
Dosage: 5 mg/kg/day
Administration: Subcutaneously implanted osmotic pump for 2 weeks
Result: Significantly decreased the blood pressure.
Clinical Trial
Molecular Weight

408.88

Formula

C20H25ClN2O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OCC)C1=C(NC(C)=C(C1C2=CC=CC=C2Cl)C(OC)=O)COCCN

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 31.25 mg/mL (76.43 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 2.4457 mL 12.2285 mL 24.4571 mL
5 mM 0.4891 mL 2.4457 mL 4.8914 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • 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)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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: ≥ 3 mg/mL (7.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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% (20% SBE-β-CD in Saline)

    Solubility: 3 mg/mL (7.34 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 3 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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:
%
DMSO +
+
%
Tween-80 +
%
Saline
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

Purity: 99.76%

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4457 mL 12.2285 mL 24.4571 mL 61.1426 mL
5 mM 0.4891 mL 2.4457 mL 4.8914 mL 12.2285 mL
10 mM 0.2446 mL 1.2229 mL 2.4457 mL 6.1143 mL
15 mM 0.1630 mL 0.8152 mL 1.6305 mL 4.0762 mL
20 mM 0.1223 mL 0.6114 mL 1.2229 mL 3.0571 mL
25 mM 0.0978 mL 0.4891 mL 0.9783 mL 2.4457 mL
30 mM 0.0815 mL 0.4076 mL 0.8152 mL 2.0381 mL
40 mM 0.0611 mL 0.3057 mL 0.6114 mL 1.5286 mL
50 mM 0.0489 mL 0.2446 mL 0.4891 mL 1.2229 mL
60 mM 0.0408 mL 0.2038 mL 0.4076 mL 1.0190 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    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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Amlodipine
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