For research use only.
CAS No. 111470-99-6
Amlodipine Besylate is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.
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Choose Selective Calcium Channel Inhibitors
|Description||Amlodipine Besylate is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.|
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. 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.  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. 
|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. |
|In vitro||DMSO||113 mg/mL (199.27 mM)|
|Ethanol||14 mg/mL (24.68 mM)|
|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.
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
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.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03371797||Completed||Drug: Valsartan Amlodipine -||Essential Hypertension||PharmEvo Pvt Ltd||February 20 2018||--|
|NCT02707913||Completed||Drug: BF-Amlodipine Tablet 10mg|Drug: Norvasc Tablet 10mg||Healthy||Bright Future Pharmaceuticals Factory O/B Bright Future Pharmaceutical Laboratories Limited|Chinese University of Hong Kong||March 2016||Phase 1|
|NCT02353806||Completed||Drug: Amlodipine besylate||Chronic Hypertension in Pregnancy||University of Texas Southwestern Medical Center|National Center for Advancing Translational Science (NCATS)||January 2015||Phase 4|
|NCT02064556||Completed||Drug: Amlodipine 10mg|Drug: Amlodipine 10mg/Candesartan 32mg||Hypertension||Chong Kun Dang Pharmaceutical||May 2014||Phase 1|
|NCT02065492||Completed||Drug: Standard Chelation|Drug: Amlodipine||Thalassemia||Aga Khan University||February 2014||Phase 2|Phase 3|
|NCT01835418||Unknown status||Drug: Amlodipine||Hypertension||Allina Health System||April 2013||Not Applicable|
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