Amlodipine Besylate

Catalog No.S1813

For research use only.

Amlodipine Besylate is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.

Amlodipine Besylate Chemical Structure

CAS No. 111470-99-6

Selleck's Amlodipine Besylate has been cited by 2 Publications

Purity & Quality Control

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Biological Activity

Description Amlodipine Besylate is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.
Targets
Calcium channel [1]
1.9 nM
In vitro

Amlodipine besylate reduces the declines in p85aPI3K, phosphorylated Akt, phosphorylated GSK-3β, heat-shock transcription factor-1, and Bcl-2 induced by H(2) O(2) , as well as the increases in cyclooxygenase-2, cytosolic cytochrome c, cleaved caspase 9, and cleaved caspase 3 in neuronal cell.[1] Amlodipine significantly reduces systolic blood pressure (SBP), 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. [2] Amlodipine elicits an NO-mediated relaxation and a leftward shift in the concentration-relaxation curve to bradykinin in isolated, pre-contracted, endothelium-intact porcine coronary arteries. Amlodipine increases the generation of NO from native endothelial cells, as detected by electron spin resonance spectroscopy and stimulated an 8-fold increase in cyclic GMP levels in cultured endothelial cells. Amlodipine elicits the NO-mediated relaxation of rat aortic rings, which do not express the B2 receptor. Amlodipine time-dependently attenuates the phosphorylation of protein kinase C (PKC) in endothelial cells, with a time course similar to the changes in eNOS phosphorylation, and prevents the phorbol-12-myristate-13-acetate-induced activation of PKC. [3]

In vivo Amlodipine besylate significantly decreases average indirect systolic blood pressure measurements from 198 mmHg to 155 mmHg in the cats. Amlodipine besylate appears to be a safe and effective oral treatment for systemic hypertension in cats when used chronically once daily as a single agent. [4]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 113 mg/mL
(199.27 mM)
Ethanol 14 mg/mL
(24.68 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

6mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 567.05
Formula

C20H25ClN2O5.C6H6O3S

CAS No. 111470-99-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC(=O)C1=C(NC(=C(C1C2=CC=CC=C2Cl)C(=O)OC)C)COCCN.C1=CC=C(C=C1)S(=O)(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04559074 Recruiting Drug: Amlodipine Hypertension Queen Mary University of London|Closed Loop Medicine Ltd|Innovate UK October 23 2020 Phase 4
NCT03722381 Withdrawn Drug: Amlodipine Besylate Hemodialysis|Pharmacokinetics University of Michigan January 2020 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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