Valsartan (CGP-48933)

For research use only.

Catalog No.S1894

3 publications

Valsartan (CGP-48933) Chemical Structure

CAS No. 137862-53-4

Valsartan (CGP-48933) is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure.

Selleck's Valsartan (CGP-48933) has been cited by 3 publications

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 (CGP-48933) purchased from Selleck.

Purity & Quality Control

Choose Selective Angiotensin Receptor Inhibitors

Biological Activity

Description Valsartan (CGP-48933) 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)
Water Insoluble
Ethanol '87 mg/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 435.52
Formula

C24H29N5O3

CAS No. 137862-53-4
Storage powder
in solvent
Synonyms N/A
Smiles CCCCC(=O)N(CC1=CC=C(C=C1)C2=CC=CC=C2C3=NNN=N3)C(C(C)C)C(=O)O

In vivo Formulation Calculator (Clear solution)

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04735354 Active not recruiting Drug: sacubitril/valsartan Heart Failure Novartis Pharmaceuticals|Novartis October 27 2020 --
NCT04753112 Recruiting Drug: Sacubitril / Valsartan Oral Tablet [Entresto] Pulmonary Hypertension Germans Trias i Pujol Hospital October 29 2020 Phase 3
NCT04128891 Withdrawn Drug: Sacubitril-Valsartan Heart Failure With Preserved Ejection Fraction Flinders University February 1 2020 Phase 3
NCT04206501 Recruiting Device: Medtronic ICD with Opti Vol-Monitor Ischemic and Non-ischemic Cardiomyopathy University of Rochester|Medtronic February 5 2020 Not Applicable

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID