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Valsartan

Valsartan

Product ID V0146
Cas No. 137862-53-4
Purity ≥98%
Product Unit SizeCostQuantityStock
50 mg $54.60 In stock
1 g $63.00 In stock
5 g $113.30 In stock
25 g $415.10 In stock
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  • Description
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Description

Valsartan is an angiotensin II (ATII) type 1 receptor (AT1) inhibitor that is clinically used to lower blood pressure and coronary resistance, and to decrease cardiac hypertrophy. Valsartan exhibits antihypertensive, cardioprotective, neuroprotective, anti-angiogenic, and anti-inflammatory activities. Inhibition of the ATII type 1 receptor results in inhibition of NF-κB and AP-1 activation. Valsartan induces autophagy through alteration of Akt/mTOR signaling in the rat heart, decreasing infarct size in an ischemia-reperfusion model. In neurons, valsartan promotes spinogenesis, increasing the number of AMPA receptors on the cell surface and altering levels of CaMKIIα and phospho-CDK5. In vivo, valsartan prevents induction of cardiotrophin-1, inhibiting increases in creatine kinase, atrial natriuretic peptide, and the heart weight/body weight ratio during heart failure. Additionally, inhibition of the angiotensin II type 1 (AT1) receptor prevents phosphorylation of Akt and decreases expression of VEGF in bone marrow stromal cells. Valsartan also inhibits release of pro-inflammatory cytokines such as IL-6, TNF-α, and IL-1β independent of its activity on ATII type 1 receptors.

Product Info

Cas No.

137862-53-4

Purity

≥98%

Formula

C24H29N5O3

Formula Wt.

435.52

Chemical Name

N-(1-Oxopentyl)-N-[[2’-1H-tetrazol-5-yl)[1,1’-biphenyl]-4-yl]methyl]-L-valine

IUPAC Name

(2S)-3-methyl-2-[pentanoyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl] methyl]amino]butanoic acid

Synonym

Diovan, Tareg

Melting Point

116-117°C

Solubility

Solubility in DMSO - 20 mg/mL. Sparingly soluble in aqueous medium.

Appearance

White to off white powder

Shipping and Storage

Store Temp

Ambient

Ship Temp

Ambient

Downloads

MSDS

V0146 MSDS PDF

Info Sheet

V0146 Info Sheet PDF

References

Wu X, He L, Cai Y, et al. Induction of autophagy contributes to the myocardial protection of valsartan against ischemia reperfusion injury. Mol Med Rep. 2013 Dec;8(6):1824-30. PMID: 24084854.

Sohn YI, Lee NJ, Chung A, et al. Antihypertensive drug Valsartan promotes dendritic spine density by altering AMPA receptor trafficking. Biochem Biophys Res Commun. 2013 Oct 4;439(4):464-70. PMID: 24012668.

Cheng CI, Hsiao CC, Wu SC, et al. Valsartan impairs angiogenesis of mesenchymal stem cells through Akt pathway. Int J Cardiol. 2013 Sep 10;167(6):2765-74. PMID: 22805546.

Al-Mazroua HA, Al-Rasheed NM, Korashy HM. Downregulation of the cardiotrophin-1 gene expression by valsartan and spironolactone in hypertrophied heart rats in vivo and rat cardiomyocyte H9c2 cell line in vitro: a novel mechanism of cardioprotection. J Cardiovasc Pharmacol. 2013 Apr;61(4):337-44. PMID: 23288202.

Iwashita M, Sakoda H, Kushiyama A, et al. Valsartan, independently of AT1 receptor or PPARγ, suppresses LPS-induced macrophage activation and improves insulin resistance in cocultured adipocytes. Am J Physiol Endocrinol Metab. 2012 Feb 1;302(3):E286-96. PMID: 22045314.

Müller DN, Mervaala EM, Dechend R, et al. Angiotensin II (AT(1)) receptor blockade reduces vascular tissue factor in angiotensin II-induced cardiac vasculopathy. Am J Pathol. 2000 Jul;157(1):111-22. PMID: 10880382.

Izumi S, Nozaki Y, Maeda K, et al. Investigation of the impact of substrate selection on in vitro organic anion transporting polypeptide 1B1 inhibition profiles for the prediction of drug-drug interactions. Drug Metab Dispos. 2015 Feb;43(2):235-247. PMID: 25414411.

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