Valsartan

Catalog No.S1894 Synonyms: CGP-48933

Valsartan Chemical Structure

Molecular Weight(MW): 435.52

Valsartan is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
USD 270 In stock
USD 570 In stock
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1 Customer Review

  • Effect of valsartan and cardamonin on Ang II-induced phosphorylation of p38 MAPK and ERK. Representative results of Western blot.

    J Nat Med 2014 68(3), 623-9. Valsartan purchased from Selleck.

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Biological Activity

Description Valsartan is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure.
Targets
angiotensin II receptor [1]
In vitro

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. [1]

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. [2] 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. [3]

Protocol

Solubility (25°C)

In vitro DMSO 87 mg/mL (199.76 mM)
Ethanol 87 mg/mL (199.76 mM)
Water Insoluble

* 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 435.52
Formula

C24H29N5O3

CAS No. 137862-53-4
Storage powder
Synonyms CGP-48933

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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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RAAS Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID