Amlodipine Besylate

Catalog No.S1813

Amlodipine Besylate Chemical Structure

Molecular Weight(MW): 567.05

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

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In DMSO USD 130 In stock
USD 97 In stock
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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

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 powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03722381 Not yet recruiting Hemodialysis|Pharmacokinetics University of Michigan December 2019 --
NCT03722381 Not yet recruiting Hemodialysis|Pharmacokinetics University of Michigan December 2019 --
NCT03683069 Not yet recruiting Hypertension|Genetics Hypertension Brigham and Women''s Hospital November 15 2019 Not Applicable
NCT03683069 Not yet recruiting Hypertension|Genetics Hypertension Brigham and Women''s Hospital November 15 2019 Not Applicable
NCT03205137 Not yet recruiting Hypertension Boehringer Ingelheim June 28 2019 --
NCT03205137 Not yet recruiting Hypertension Boehringer Ingelheim June 28 2019 --

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Calcium Channel Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID