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Valsartan Angiotensin Receptor antagonist

Name: Valsartan
Brand: Selleck Chemicals
SKU: S1894
Availability: InStock
Rating: 5 (6 reviews)

Cat.No.S1894

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

Chemical Structure

Molecular Weight: 435.52

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.89%

99.89

Related Targets	Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras GPR GluR Prostaglandin Receptor CXCR Adenosine Receptor P2 Receptor CCR Hedgehog/Smoothened S1P Receptor PKA Cannabinoid Receptor cAMP Glucagon Receptor SGLT Opioid Receptor Sigma Receptor PAR Endothelin Receptor LTR Neurokinin Receptor Guanylate Cyclase PKG LPA Receptor OX Receptor
Related Products	PD123319 ML221 A-779 Fimasartan Olodanrigan (EMA401) Buloxibutid

Chemical Information, Storage & Stability

Molecular Weight	435.52	Formula	C₂₄H₂₉N₅O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	137862-53-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CGP-48933			Smiles	CCCCC(=O)N(CC1=CC=C(C=C1)C2=CC=CC=C2C3=NNN=N3)C(C(C)C)C(=O)O

Solubility

In vitro
Batch:

DMSO : 87 mg/mL (199.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 87 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.350mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 87 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.725mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 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.

Mechanism of Action

Targets/IC₅₀/Ki	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. This compound 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. This compound treatment also blocks Western diet-induced increases in serum levels of the proinflammatory cytokines interferon-gamma and monocyte chemotactic protein 1. It enhances mitochondrial function and prevents Western diet-induced decreases in glucose-stimulated insulin secretion in the pancreatic islets of mice. This 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] It 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. This chemical 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. It also reduces tumor necrosis factor-alpha (TNF-alpha) expression and superoxide production in skeletal muscle of KK-Ay mice. ^[3]
References	[1] https://pubmed.ncbi.nlm.nih.gov/15991938/ [2] https://pubmed.ncbi.nlm.nih.gov/20100990/ [3] https://pubmed.ncbi.nlm.nih.gov/15037562/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05989503	Recruiting	Heart Failure With Reduced Ejection Fraction	Universidade do Porto\|Unidade de Investigação e Desenvolvimento Cardiovascular (UnIC)\|Rede de Investigação em Saúde	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	August 11 2022	Phase 1\|Phase 2

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