Catalog No.S1894 Synonyms: CGP-48933
Molecular Weight(MW): 435.52
Valsartan is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure.
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|Description||Valsartan is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure.|
Valsartan dose-dependently inhibits the vasoconstriction induced by angiotensin II and lowers blood pressure in renin-dependent models of hypertension. Valsartan is at least as effective as ACE inhibitors, diuretics, beta-blockers and calcium antagonists. 
|In vivo||Valsartan results in improved glucose tolerance, reduced fasting blood glucose levels, and reduced serum insulin levels in mice fed a Western diet. Valsartan treatment also blocks Western diet-induced increases in serum levels of the proinflammatory cytokines interferon-gamma and monocyte chemotactic protein 1. Valsartan enhances mitochondrial function and prevents Western diet-induced decreases in glucose-stimulated insulin secretion in the pancreatic islets of mice. Valsartan treatment blocks or attenuates Western diet-induced changes in expression of several key inflammatory signals: interleukin 12p40, interleukin 12p35, tumor necrosis factor-alpha, interferon-gamma, adiponectin, platelet 12-lipoxygenase, collagen 6, inducible NO synthase, and AT1R in isolated adipocytes.  Valsartan significantly increases insulin-mediated 2-[3H]deoxy-d-glucose (2-[3H]DG) uptake into skeletal muscle and attenuates the increase in plasma glucose concentration after a glucose load and plasma concentrations of glucose and insulin. Valsartan treatment exaggerates the insulin-induced phosphorylation of IRS-1, the association of IRS-1 with the p85 regulatory subunit of phosphoinositide 3 kinase (PI 3-K), PI 3-K activity, and translocation of GLUT4 to the plasma membrane. Valsartan also reduces tumor necrosis factor-alpha (TNF-alpha) expression and superoxide production in skeletal muscle of KK-Ay mice. |
|In vitro||DMSO||87 mg/mL (199.76 mM)|
|Ethanol||87 mg/mL (199.76 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02662894||Not yet recruiting||Hypertension|Dyslipidemia||EMS||July 2017||Phase 3|
|NCT02816736||Not yet recruiting||Heart Failure||Duke University|National Heart, Lung, and Blood Institute (NHLBI)||February 2017||Phase 4|
|NCT03005184||Recruiting||Heart Failure NYHA Class I|Heart Failure NYHA Class II|Heart Failure NYHA Class III||Vanderbilt University Medical Center||January 2017||--|
|NCT01805804||Recruiting||First Time Dual Chamber Pacemaker Implantation||Medical University of Silesia|Polpharma Pharmaceutical Company||January 2017||Phase 4|
|NCT02924727||Recruiting||Acute Myocardial Infarction||Novartis Pharmaceuticals|Novartis||December 2016||Phase 3|
|NCT02900378||Recruiting||Chronic Heart Failure With Reduced Ejection Fraction||Novartis Pharmaceuticals|Novartis||December 2016||Phase 3|
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