Home Transmembrane Transporters Calcium Channel inhibitor Amlodipine Besylate For research use only.

Amlodipine Besylate

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

Amlodipine Besylate Chemical Structure

Amlodipine Besylate Chemical Structure

CAS: 111470-99-6

Selleck's Amlodipine Besylate has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.97%
99.97

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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
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
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]

Chemical lnformation & Solubility

Molecular Weight 567.05 Formula

C20H25ClN2O5.C6H6O3S
CAS No. 111470-99-6 SDF Download Amlodipine Besylate SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 113 mg/mL ( (199.27 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble


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In vivo
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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.

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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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