Valsartan | CAS#137862-53-4 | Angiotensin II Receptor Antagonist

MedKoo Cat#: 318970 | Name: Valsartan

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Valsartan is an angiotensin II receptor antagonist (commonly called an ARB, or angiotensin receptor blocker), that is selective for the type I (AT1) angiotensin receptor. Valsartan is mainly used for treatment of high blood pressure, congestive heart failure, and to increase the chances of living longer after a heart attack. Valsartan is used to treat high blood pressure, congestive heart failure, and to reduce death for people with left ventricular dysfunction after having had a heart attack.

Chemical Structure

Valsartan

CAS#137862-53-4

Theoretical Analysis

MedKoo Cat#: 318970

Name: Valsartan

CAS#: 137862-53-4

Chemical Formula: C24H29N5O3

Exact Mass: 435.2270

Molecular Weight: 435.53

Elemental Analysis: C, 66.19; H, 6.71; N, 16.08; O, 11.02

Price and Availability

Size	Price	Availability
500mg	USD 150.00	Ready to ship
1g	USD 250.00	Ready to ship
2g	USD 400.00	Ready to ship
5g	USD 750.00	Ready to ship
10g	USD 1,250.00	Ready to ship

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Related CAS #

936623-90-4 137862-53-4 149690-05-1 (sodium)

Synonym

CGP48933, CGP-48933, CGP 48933, Valsartan, Diovan, Miten, Nisis, Prova, Tareg, Vals, Walsartan

IUPAC/Chemical Name

(S)-3-methyl-2-(N-{[2'-(2H-1,2,3,4-tetrazol-5-yl)biphenyl-4-yl]methyl}pentanamido)butanoic acid

InChi Key

ACWBQPMHZXGDFX-QFIPXVFZSA-N

InChi Code

InChI=1S/C24H29N5O3/c1-4-5-10-21(30)29(22(16(2)3)24(31)32)15-17-11-13-18(14-12-17)19-8-6-7-9-20(19)23-25-27-28-26-23/h6-9,11-14,16,22H,4-5,10,15H2,1-3H3,(H,31,32)(H,25,26,27,28)/t22-/m0/s1

SMILES Code

CC(C)[C@H](N(CC1=CC=C(C2=CC=CC=C2C3=NNN=N3)C=C1)C(CCCC)=O)C(O)=O

Appearance

White to off-white crystalline powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Note: This product has also cat#558302

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#BBC60919

QC Data

View QC data: current batch, Lot#BBC60919

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

Valsartan (CGP 48933) is an angiotensin II receptor antagonist.

In vitro activity:

Exposure of HPMCs to AngII increased the protein expression levels of p-mTOR, p-4EBP1, and p-S6K1, as assessed by Western blot, and HG had the similar role as the AngII. Cotreatment with valsartan ameliorated the HG-induced or AngII-induced upregulation of components of the mTORC1 pathway (Figure 6(a) and (b)). To further determine the mechanisms associated with the regulation of ECM accumulation by valsartan, this study subsequently analyzed the effect of the speciﬁc mTOR agonist MHY1485 on valsartan-mediated α-SMA and collagen I expression. The data showed that, compared with valsartan, MHY1485 dramatically increased the expression of α-SMA and collagen I, even in the presence of valsartan, as determined by Western blot (Figure 6(c)and (d)). Taken together, these results suggest that the protective effect of valsartan against PF is related to the downregulation of the activity of the mTORC1 pathway. Reference: Exp Biol Med (Maywood). 2020 Jun; 245(11): 983–993. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7427179/

In vivo activity:

The results of the current study indicated that: 1) valsartan at a dose of 20 mg/kg/day treated balloon injured rats for both 14 and 28 days significantly inhibited the neointimal hyperplasia and reduced the aortic SRSF1 expression; 2) valsartan decreased the aortic angiotensin II and iNOS levels while increased the aortic eNOS level; and 3) valsartan downregulated the TLR4 and AT1 receptor while upregulated the AT2 receptor mRNA and protein expression. Valsartan also decreased the aortic p-ERK protein expression. These findings suggest that the therapeutic potential of valsartan in attenuating neointimal hyperplasia and inhibiting the TLR4-iNOS-ERK-AT1 receptor pathway and SRSF1 expression in balloon-injured rat aorta. Reference: Physiol Res. 2021 Jun 1. https://pubmed.ncbi.nlm.nih.gov/34062069/

	Solvent	mg/mL	mM
Solubility
	Ethanol	30.0	68.88
	Ethanol:PBS (pH 7.2) (1:1)	0.5	1.15
	Water	87.0	499.76

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 435.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Liu J, Feng Y, Sun C, Zhu W, Zhang QY, Jin B, Shao QY, Xia YY, Xu PF, Zhang M, Jiang CM. Valsartan ameliorates high glucose-induced peritoneal ﬁbrosis by blocking mTORC1 signaling. Exp Biol Med (Maywood). 2020 Jun;245(11):983-993. doi: 10.1177/1535370220919364. Epub 2020 May 14. PMID: 32408765; PMCID: PMC7427179. 2. Sui X, Wei H, Wang D. Novel mechanism of cardiac protection by valsartan: synergetic roles of TGF-β1 and HIF-1α in Ang II-mediated fibrosis after myocardial infarction. J Cell Mol Med. 2015 Aug;19(8):1773-82. doi: 10.1111/jcmm.12551. Epub 2015 Mar 30. PMID: 25823960; PMCID: PMC4549028. 3. Li Y, Guo J, Yu H, Liu X, Zhou J, Chu X, Xu Q, Sun T, Peng L, Yang X, Tang X. Valsartan Prevented Neointimal Hyperplasia and Inhibited SRSF1 Expression and the TLR4-iNOS-ERK-AT1 Receptor Pathway in the Balloon-injured Rat Aorta. Physiol Res. 2021 Jun 1. Epub ahead of print. PMID: 34062069. 4. Tehrani AY, White Z, Milad N, Esfandiarei M, Seidman MA, Bernatchez P. Blood pressure-independent inhibition of Marfan aortic root widening by the angiotensin II receptor blocker valsartan. Physiol Rep. 2021 May;9(10):e14877. doi: 10.14814/phy2.14877. PMID: 34042309; PMCID: PMC8157789.

In vitro protocol:

In vivo protocol:

1. Li Y, Guo J, Yu H, Liu X, Zhou J, Chu X, Xu Q, Sun T, Peng L, Yang X, Tang X. Valsartan Prevented Neointimal Hyperplasia and Inhibited SRSF1 Expression and the TLR4-iNOS-ERK-AT1 Receptor Pathway in the Balloon-injured Rat Aorta. Physiol Res. 2021 Jun 1. Epub ahead of print. PMID: 34062069. 2. Tehrani AY, White Z, Milad N, Esfandiarei M, Seidman MA, Bernatchez P. Blood pressure-independent inhibition of Marfan aortic root widening by the angiotensin II receptor blocker valsartan. Physiol Rep. 2021 May;9(10):e14877. doi: 10.14814/phy2.14877. PMID: 34042309; PMCID: PMC8157789.

1: Hasabo EA, Isik B, Elgadi A, Yacoub MS, Bakr MS, Eljack MMF, Sultan S, Caliskan K, Soliman O. A Systematic Review and Meta-Analysis of an Angiotensin Receptor-Neprilysin Inhibitor in Patients Using a Durable Left Ventricular Assist Device. J Clin Med. 2024 Dec 20;13(24):7789. doi: 10.3390/jcm13247789. PMID: 39768713. 2: Ciriello GD, Altobelli I, Fusco F, Colonna D, Correra A, Papaccioli G, Romeo E, Scognamiglio G, Sarubbi B. Sacubitril/Valsartan and Dapagliflozin in Patients with a Failing Systemic Right Ventricle: Effects on the Arrhythmic Burden. J Clin Med. 2024 Dec 16;13(24):7659. doi: 10.3390/jcm13247659. PMID: 39768582. 3: Hajahmadi M, Zeinali E, Joghataie P, Pazoki M. Comparison of the effect of Sacubitril/Valsartan with Losartan and Captopril in improving right ventricular function in patients with right heart failure, a randomized clinical controlled trial. J Prev Med Hyg. 2024 Oct 31;65(3):E395-E402. doi: 10.15167/2421-4248/jpmh2024.65.3.3305. PMID: 39758759; PMCID: PMC11698105. 4: Abumayyaleh M, Krack C, Demmer J, Pilsinger C, Schupp T, Behnes M, Sattler K, El-Battrawy I, Hamdani N, Akin I. Sex differences and clinical outcomes, including ventricular tachyarrhythmias, of patients with heart failure with reduced ejection fraction treated with sacubitril/valsartan. Front Cardiovasc Med. 2024 Dec 19;11:1503414. doi: 10.3389/fcvm.2024.1503414. PMID: 39749312; PMCID: PMC11693701. 5: Perry B, Jakab J, Robinson B, McElhaney E, Fallon J, Geyer K. Implementation of an adherence pharmacy referral protocol for patients taking sacubitril/valsartan. J Manag Care Spec Pharm. 2025 Jan;31(1):83-87. doi: 10.18553/jmcp.2025.31.1.83. PMID: 39745848; PMCID: PMC11695842. 6: Lu H, Kondo T, Claggett BL, Vaduganathan M, Neuen BL, Beldhuis IE, Jhund PS, Mc Causland FR, Anand IS, Pfeffer MA, Pitt B, Zannad F, Zile MR, McMurray JJV, Solomon SD, Desai AS. Systolic Blood Pressure and Pulse Pressure in Heart Failure: Pooled Participant-Level Analysis of 4 Trials. J Am Coll Cardiol. 2024 Nov 15:S0735-1097(24)10420-2. doi: 10.1016/j.jacc.2024.11.007. Epub ahead of print. PMID: 39745404. 7: Zhu X, Li X, Zhu L, Tong Z, Xu X. Angiotensin Receptor-Neprilysin Inhibitor in Heart Failure Patients With Renal Dysfunction. Cardiovasc Ther. 2024 Nov 4;2024:6231184. doi: 10.1155/2024/6231184. PMID: 39742017; PMCID: PMC11554417. 8: Wang N, Wang H, Chen Y, Wang Y. A real-world pharmacovigilance analysis of potential ototoxicity associated with sacubitril/valsartan based on FDA Adverse Event Reporting System (FAERS). Sci Rep. 2024 Dec 30;14(1):31591. doi: 10.1038/s41598-024-79272-8. PMID: 39738184; PMCID: PMC11686400. 9: Liu K, Xiong Y, Fan Y, Li S, Wu L, Chen H, Wang X. Research on the mechanism of the anti-myocardial infarction effect of the Qiliqiangxin capsule on heart failure rats via nontargeted metabolomics and lipidomics. BMC Cardiovasc Disord. 2024 Dec 31;24(1):762. doi: 10.1186/s12872-024-04423-8. PMID: 39736521; PMCID: PMC11686870. 10: Liu DH, Dong XM, Long WJ. Advancing cardiovascular outcomes with dapagliflozin and sacubitril in post-acute myocardial infarction heart failure and type 2 diabetes mellitus. World J Clin Cases. 2024 Dec 26;12(36):6935-6938. doi: 10.12998/wjcc.v12.i36.6935. PMID: 39726920; PMCID: PMC11531987. 11: Zhao Y, Jia Q, Hao G, Han L, Gao Y, Zhang X, Yan Z, Li B, Wu Y, Zhang B, Li Y, Qin J. JiangyaTongluo decoction ameliorates tubulointerstitial fibrosis via regulating the SIRT1/PGC-1α/mitophagy axis in hypertensive nephropathy. Front Pharmacol. 2024 Dec 12;15:1491315. doi: 10.3389/fphar.2024.1491315. PMID: 39726785; PMCID: PMC11669701. 12: Inarmal N, Moodley B. Removal efficiencies and environmental risk assessment of selected pharmaceuticals and metabolites at a wastewater treatment plant in Pietermaritzburg, South Africa. Environ Monit Assess. 2024 Dec 26;197(1):102. doi: 10.1007/s10661-024-13515-z. PMID: 39724437; PMCID: PMC11671546. 13: Mahmood NMS, Mahmud AMR, Maulood IM. Melatonin attenuates responses to angiotensin II in isolated aortic rings of STZ-induced type 1-like DM rats. Endocr Res. 2024 Dec 24:1-13. doi: 10.1080/07435800.2024.2445264. Epub ahead of print. PMID: 39719865. 14: Lu H, Inciardi RM, Abanda M, Shah AM, Cikes M, Claggett BL, Prasad N, Lam CSP, Redfield M, McMurray JJV, Pfeffer MA, Solomon SD, Hegde SM, Skali H. Multiparametric Assessment of Right Ventricular Dysfunction in Heart Failure: An Analysis From PARAGON-HF. J Am Heart Assoc. 2024 Dec 24:e037380. doi: 10.1161/JAHA.124.037380. Epub ahead of print. PMID: 39719412. 15: Solano S, Yang M, Tolomeo P, Kondo T, Shen L, Jhund PS, Anand IS, Desai AS, Lam CSP, Maggioni AP, Martinez FA, Rouleau JL, Vaduganathan M, van Veldhuisen DJ, Zannad F, Zile MR, Packer M, Solomon SD, McMurray JJV. Clinical Characteristics and Outcomes of Patients With Heart Failure With Preserved Ejection Fraction and With Reduced Ejection Fraction According to the Prognostic Nutritional Index: Findings From PARADIGM-HF and PARAGON-HF. J Am Heart Assoc. 2024 Dec 24:e037782. doi: 10.1161/JAHA.124.037782. Epub ahead of print. PMID: 39719408. 16: Akinmoju OD, Olatunji G, Kokori E, Ogieuhi IJ, Babalola AE, Obi ES, Anthony CS, Toluwanibukun OG, Akingbola A, Alao AE, Boluwatife AG, Venkatraman A, Babar A, Aderinto N. Comparative Efficacy of Continuous Positive Airway Pressure and Antihypertensive Medications in Obstructive Sleep Apnea-Related Hypertension: A Narrative Review. High Blood Press Cardiovasc Prev. 2024 Dec 24. doi: 10.1007/s40292-024-00691-9. Epub ahead of print. PMID: 39718706. 17: Zhao L, Ren Y, Qin D, Yang X, Chen Z, Zhang N. Retrospective Analysis of Sacubitril/Valsartan vs Benazepril for Treating Heart Failure Following Acute Myocardial Infarction. Int J Gen Med. 2024 Dec 19;17:6367-6376. doi: 10.2147/IJGM.S496996. PMID: 39717069; PMCID: PMC11665437. 18: Kow CS, Ramachandram DS, Hasan SS, Thiruchelvam K. Rethinking angiotensin receptor blocker (ARB) use in COVID-19: a class-wide call for careful dosing. Hypertens Res. 2024 Dec 23. doi: 10.1038/s41440-024-02055-1. Epub ahead of print. PMID: 39715790. 19: Kontham R, Sadanande MV, Thorat SS, Sharma H, Singh G, Vanka K, Gonnade RG. Studies on the Stereoselective Synthesis of Sacubitril via a Chiral Amine Transfer Approach. Chem Asian J. 2024 Dec 23:e202401223. doi: 10.1002/asia.202401223. Epub ahead of print. PMID: 39714458. 20: Nordén ES, Bendiksen BA, Bergo KK, Espe EKS, McGinley G, Hasic A, Hauge- Iversen IM, Ugland HK, Shen X, Frisk M, Mabotuwana NS, Louch WE, Hussain RI, Zhang L, Sjaastad I, Cataliotti A, Christensen G. Sacubitril/valsartan preserves regional cardiac function following myocardial infarction in rats. ESC Heart Fail. 2024 Dec 18. doi: 10.1002/ehf2.15145. Epub ahead of print. PMID: 39696842.