Amlodipine (UK-48340; Norvasc)

Alias: UK-48340; mlodis; Norvasc; Amlocard; Coroval;UK 48340; Amlodipine Besylate; Amlodipine Maleate;UK48340; Amlodipine Maleate
Cat No.:V0650 Purity: ≥98%
Amlodipine (formerly UK48340; trade name Norvasc among others), a marketed antihypertensive drug, is a long-acting L-type calcium channel blocker/CCB of the dihydropyridine/DHP class.
Amlodipine (UK-48340; Norvasc) Chemical Structure CAS No.: 88150-42-9
Product category: Calcium Channel
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
2g
5g
10g
Other Sizes

Other Forms of Amlodipine (UK-48340; Norvasc):

  • Amlodipine maleate
  • Amlodipine Besylate (Norvasc)
  • Amlodipine mesylate
  • Amlodipine-1,1,2,2-d4 maleate (Amlodipine d4 (maleate))
  • Amlodipine-d4 (Amlodipine-d4)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Amlodipine (formerly UK48340; trade name Norvasc among others), a marketed antihypertensive drug, is a long-acting L-type calcium channel blocker/CCB of the dihydropyridine/DHP class. It is an approved medication that has been widely used to treat high blood pressure.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In A431 cells, amlodipine (20–40 μM; 48 h) decreases BrdU incorporation to 68.6% and 26.3% at 20 and 30 μM, respectively[3]. Amlodipine (30 μM; pretreatment for 1 h) greatly reduces the increases in [Ca2+]i in A431 cells caused by uridine 5′-triphosphate (UTP)[3]. In cells loaded with Fluo-3, amlodipine (30 μM) suppresses the store-operated Ca2+influx triggered by thapsigargin[3].
ln Vivo
In VSMC ATP2B1 KO mice, amlodipine (5 mg/kg/day; sc for 2 weeks) significantly lowers systolic blood pressure (SBP)[4]. ?Amlodipine (10 mg/kg; intraperitoneal; once daily for 20 days) significantly slows the formation of tumors and increases the longevity of A431 tumor-bearing mice[3].
Animal Protocol
Animal/Disease Models: ATP2B1loxP/loxP mice[4]
Doses: 5 mg/kg/day
Route of Administration: subcutaneously (sc) implanted osmotic pump for 2 weeks
Experimental Results: Dramatically diminished the blood pressure.
References
[1]. Kishen G. Bulsara, et al. Amlodipine.
[2]. Haria M, et al. Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease [published correction appears in Drugs 1995 Nov;50(5):896]. Drugs. 1995;50(3):560-586.
[3]. Yoshida J, et, al. Antitumor effects of amlodipine, a Ca2+ channel blocker, on human epidermoid carcinoma A431 cells in vitro and in vivo. Eur J Pharmacol. 2004 May 25;492(2-3):103-12.
[4]. Okuyama Y, et, al. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H25CLN2O5
Molecular Weight
408.88
CAS #
88150-42-9
Related CAS #
Amlodipine maleate;88150-47-4;Amlodipine besylate;111470-99-6;Amlodipine mesylate;246852-12-0;Amlodipine-1,1,2,2-d4 maleate;1185246-15-4;Amlodipine-d4;1185246-14-3
SMILES
ClC1=C([H])C([H])=C([H])C([H])=C1C1([H])C(C(=O)OC([H])([H])[H])=C(C([H])([H])[H])N([H])C(C([H])([H])OC([H])([H])C([H])([H])N([H])[H])=C1C(=O)OC([H])([H])C([H])([H])[H]
Synonyms
UK-48340; mlodis; Norvasc; Amlocard; Coroval;UK 48340; Amlodipine Besylate; Amlodipine Maleate;UK48340; Amlodipine Maleate
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)
Solubility Data
Solubility (In Vitro)
DMSO:82 mg/mL (200.5 mM)
Water:< 1 mg/mL
Ethanol:82 mg/mL (200.5 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 3 mg/mL (7.34 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 30.0 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: 3 mg/mL (7.34 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 3 mg/mL (7.34 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 30.0 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 2.4457 mL 12.2285 mL 24.4571 mL
5 mM 0.4891 mL 2.4457 mL 4.8914 mL
10 mM 0.2446 mL 1.2229 mL 2.4457 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT06193044 Not yet recruiting Drug:Amlodipine/Valsartan Healthy Volunteer International Bio service May 7, 2024 Phase 1
NCT01835418 Unknown Drug:Amlodipine Hypertension Allina Health System April 2013 Not Applicable
NCT04554303 Unknown Drug: S-amlodipine 2.5mg
Drug: Amlodipine 5mg
Essential Hypertension Ahn-Gook Pharmaceuticals Co.,Ltd October 28, 2020
NCT03294070 Unknown Arterial Hypertension Recurrent Glioma
Refractory Glioma
Centro Universitario de
Ciencias de la Salud, Mexico
September 2017 Phase 4
NCT05667818 Not yet recruiting Drug: Amlodipine besylate tablets Hypertension Overseas Pharmaceuticals, Ltd. January 28, 2023 Phase 1
Biological Data
  • Changes in SBP produced by a single injection of anti-hypertensive drugs. (a) Delta SBP in response to the administration of nicardipine (1 mg kg−1, i.p., n=7 for each group). (b) Delta SBP in response to the administration of candesartan (10 mg kg−1, i.p., n=8 for each group). (c) Delta SBP in response to the administration of prazosin (1 mg kg−1, i.p., n=6 for each group). (d) Delta SBP in response to the administration of amlodipine (5 mg kg−1, i.p., n=8 for each group). (e) Delta SBP in response to the administration of nicardipine every 6 h. The data are means±s.e.m. of each group. *P<0.05 vs. the control group. **P<0.01 vs. the control group. Each arrow indicates the time of drug injection. A horizontal line shows the time after (or before) injection and each injection was at ~15:00. C, control mice; K, VSMC ATP2B1 KO mice. Hypertens Res . 2018 Feb;41(2):80-87.
  • SBP shifts produced by long-term administration of amlodipine and candesartan measured by the tail-cuff method. (a) SBP and (b) Delta SBP from the baseline in mice administered amlodipine for 2 weeks (5 mg kg−1 per day, s.c., n=9 for each group). (c) SBP and (d) Delta SBP from the baseline in mice administered candesartan for 2 weeks (0.5 mg kg−1 per day, s.c., n=7 for each group). The data are means±s.e.m. of group. *P<0.05 vs. the control group. #P<0.05 vs. own baseline. Hypertens Res . 2018 Feb;41(2):80-87.
  • SBP shifts produced by amlodipine administration on days 2, 3, 7, and 14 were examined by radio telemetric measurement. (a) Changes in delta SBP of mice treated with amlodipine (5 mg kg−1 per day, s.c., n=6–8). Circadian patterns of SBP of (b) Control and (c) VSMC ATP2B1 KO mice treated with amlodipine for 1 week, measured by the radio telemetric method. Basal SBPs were also measured (n=6–8). 12-h light (8:00 AM to 20:00 PM)/dark (20:00 PM to 8:00 AM) cycle are shown. Values plotted are hourly means. Data are means±s.e.m. of group. *P<0.05 vs. the control group. Hypertens Res . 2018 Feb;41(2):80-87.
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