Home GPCR & G Protein Angiotensin Receptor antagonist Valsartan For research use only.

Valsartan

Synonyms: CGP-48933

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

Valsartan Chemical Structure

Valsartan Chemical Structure

CAS: 137862-53-4

Selleck's Valsartan has been cited by 4 Publications

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Purity & Quality Control

Batch: Purity: 100%
100

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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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05989503 Recruiting Heart Failure With Reduced Ejection Fraction Universidade do Porto|Faculty of Medicine (FMUP)|Unidade de Investigação e Desenvolvimento Cardiovascular (UnIC)|Rede de Investigação em Saúde (RISE) Laboratório Associado August 4 2023 Phase 4
NCT05870709 Withdrawn Heart Failure Novartis Pharmaceuticals|Novartis May 15 2023 --
NCT05564572 Enrolling by invitation Heart Failure Stanford University September 7 2022 Not Applicable
NCT05194111 Recruiting Heart Failure|Heart Dysfunction Virginia Commonwealth University March 9 2022 Phase 1|Phase 2

Chemical lnformation & Solubility

Molecular Weight 435.52 Formula

C24H29N5O3
CAS No. 137862-53-4 SDF Download Valsartan SDF
Smiles CCCCC(=O)N(CC1=CC=C(C=C1)C2=CC=CC=C2C3=NNN=N3)C(C(C)C)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 87 mg/mL ( (199.76 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 87 mg/mL

Water : Insoluble


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In vivo
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