Amlodipine Calcium Channel inhibitor

Cat.No.S1905

Amlodipine (UK-48340) is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.
Amlodipine  Calcium Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 408.88

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 408.88 Formula

C20H25ClN2O5

Storage (From the date of receipt)
CAS No. 88150-42-9 Download SDF Storage of Stock Solutions

Synonyms UK-48340 Smiles CCOC(=O)C1=C(NC(=C(C1C2=CC=CC=C2Cl)C(=O)OC)C)COCCN

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (200.54 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 82 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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mg/kg g μL

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%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Calcium channel [1]
In vitro
Amlodipine causes a dose-dependent increase in nitrite production. This compound also increases nitrite production in large coronary arteries and in aorta. [1] It is attributed to distinct membrane physico-chemical interactions. This chemical contributes to distinct membrane biophysical interactions that lead to potent lipid antioxidant effects, independent of calcium channel modulation. [2] It increases plaque smooth muscle cell content (P<0.05), whereas atenolol decreases plaque inflammation. [3] This compound attenuates intracellular neuronal Ca2+ increases elicited by KCl depolarization but does not affect Ca2+ changes triggered by N-methyl-D-aspartate receptor activation. It also inhibits free radical-induced damage to lipid constituents of the membrane in a dose-dependent manner, independent of Ca2+ channel modulation. [4]
In vivo
Amlodipine results in regression of cardiovascular hypertrophy and amelioration of endothelial dysfunction in spontaneously hypertensive rats. [5] This compound significantly reduces aortic hypertrophy, endothelial dysfunction, LOX-1 expression, aortic O(2)(-) and ONOO(-) production, and plasma free 8-F(2)alpha-isoprostane levels in Ang II-infused rats. It has antihypertensive and antioxidant activity in vivo, which effectively inhibits many of the oxidative stress-dependent mechanisms involved in Ang II-mediated cardiovascular injury. [6]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/10098848/
  • [5] https://pubmed.ncbi.nlm.nih.gov/9797191/
  • [6] https://pubmed.ncbi.nlm.nih.gov/14751660/

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