Valsartan
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MedKoo CAT#: 318970

CAS#: 137862-53-4

Description: 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

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Valsartan
CAS# 137862-53-4

Theoretical Analysis

MedKoo Cat#: 318970
Name: Valsartan
CAS#: 137862-53-4
Chemical Formula: C24H29N5O3
Exact Mass: 435.23
Molecular Weight: 435.528
Elemental Analysis: C, 66.19; H, 6.71; N, 16.08; O, 11.02

Price and Availability

Size Price Availability Quantity
500mg USD 150 Ready to ship
1g USD 250 Ready to ship
2g USD 400 Ready to ship
5g USD 750 Ready to ship
10g USD 1250 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

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/

Solubility Data

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

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.

Recalculate based on batch purity %
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: 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.
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.

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1: Lillyblad MP. Dual Angiotensin Receptor and Neprilysin Inhibition with Sacubitril/Valsartan in Chronic Systolic Heart Failure: Understanding the New PARADIGM. Ann Pharmacother. 2015 Nov;49(11):1237-51. doi: 10.1177/1060028015593093. Epub 2015 Jul 14. Review. PubMed PMID: 26175499.

2: Ardiana F, Suciati, Indrayanto G. Valsartan. Profiles Drug Subst Excip Relat Methodol. 2015;40:431-93. doi: 10.1016/bs.podrm.2015.01.004. Epub 2015 Mar 21. Review. PubMed PMID: 26051690.

3: Janić M, Lunder M, Šabovič M. A low-dose combination of fluvastatin and valsartan: a new "drug" and a new approach for decreasing the arterial age. Biomed Res Int. 2015;2015:235709. doi: 10.1155/2015/235709. Epub 2015 Mar 3. Review. PubMed PMID: 25821790; PubMed Central PMCID: PMC4363554.

4: Sander GE, Giles TD. Nebivolol and valsartan as a fixed-dose combination for the treatment of hypertension. Expert Opin Pharmacother. 2015 Apr;16(5):763-70. doi: 10.1517/14656566.2015.1020790. Review. PubMed PMID: 25747524.

5: Güleç S. Valsartan after myocardial infarction. Anadolu Kardiyol Derg. 2014 Dec;14 Suppl 2:S9-13. doi: 10.5152/akd.2014.00002. Review. PubMed PMID: 25604205.

6: Kızılırmak P, Üresin AY. Hypertension and valsartan. Anadolu Kardiyol Derg. 2014 Dec;14 Suppl 2:S20-4. doi: 10.5152/akd.2014.00004. Review. PubMed PMID: 25604204.

7: Ecder T. Renal and metabolic effects of valsartan. Anadolu Kardiyol Derg. 2014 Dec;14 Suppl 2:S14-9. doi: 10.5152/akd.2014.00003. Review. PubMed PMID: 25604203.

8: Kılıçkıran Avcı B, İkitimur B, Karadağ B, Öngen Z. Renin-angiotensin system blockade in the treatment of heart failure and the role of valsartan in this treatment. Anadolu Kardiyol Derg. 2014 Dec;14 Suppl 2:S1-8. doi: 10.5152/akd.2014.00001. Review. PubMed PMID: 25604202.

9: Varagic J, Punzi H, Ferrario CM. Clinical utility of fixed-dose combinations in hypertension: evidence for the potential of nebivolol/valsartan. Integr Blood Press Control. 2014 Nov 26;7:61-70. doi: 10.2147/IBPC.S50954. eCollection 2014. Review. PubMed PMID: 25473311; PubMed Central PMCID: PMC4251532.

10: Lawrence Gould A, Unniachan S, Wu D. Indirect treatment comparison between fixed-dose-combinations of amlodipine/losartan and amlodipine/valsartan in blood pressure control. Int J Clin Pract. 2014 Feb;68(2):163-72. doi: 10.1111/ijcp.12343. Review. PubMed PMID: 24460615.

11: Huang QF, Li Y, Wang JG. Overview of clinical use and side effect profile of valsartan in Chinese hypertensive patients. Drug Des Devel Ther. 2013 Dec 30;8:79-86. doi: 10.2147/DDDT.S38617. Review. PubMed PMID: 24403822; PubMed Central PMCID: PMC3883632.

12: Ferdinand KC, Nasser SA. A review of the efficacy and tolerability of combination amlodipine/valsartan in non-white patients with hypertension. Am J Cardiovasc Drugs. 2013 Oct;13(5):301-13. doi: 10.1007/s40256-013-0033-4. Review. PubMed PMID: 23784267; PubMed Central PMCID: PMC3781303.

13: Voors AA, Dorhout B, van der Meer P. The potential role of valsartan + AHU377 ( LCZ696 ) in the treatment of heart failure. Expert Opin Investig Drugs. 2013 Aug;22(8):1041-7. doi: 10.1517/13543784.2013.797963. Epub 2013 May 10. Review. PubMed PMID: 23663006.

14: Volpe M. Preventing cardiovascular events with angiotensin II receptor blockers: a closer look at telmisartan and valsartan. Expert Rev Cardiovasc Ther. 2012 Aug;10(8):1061-72. doi: 10.1586/erc.12.80. Review. PubMed PMID: 23030295.

15: Benge CD, Muldowney JA 3rd. The pharmacokinetics and pharmacodynamics of valsartan in the post-myocardial infarction population. Expert Opin Drug Metab Toxicol. 2012 Nov;8(11):1469-82. doi: 10.1517/17425255.2012.725721. Epub 2012 Sep 24. Review. PubMed PMID: 22998368.

16: Lacourcière Y. Telmisartan or valsartan alone or in combination with hydrochlorothiazide: a review. Clin Exp Hypertens. 2013;35(1):50-60. doi: 10.3109/10641963.2012.690468. Epub 2012 Aug 6. Review. PubMed PMID: 22866964.

17: Miura S, Saku K. Efficacy and safety of angiotensin II type 1 receptor blocker/calcium channel blocker combination therapy for hypertension: focus on a single-pill fixed-dose combination of valsartan and amlodipine. J Int Med Res. 2012;40(1):1-9. Review. PubMed PMID: 22429340.

18: Sestito A. Hypertension therapy and cardiovascular protection. Effects of angiotensin II receptor block with Valsartan. Eur Rev Med Pharmacol Sci. 2011 Nov;15(11):1247-55. Review. PubMed PMID: 22195356.

19: Maksimov ML, Mochkin IA, Starodubtsev AK. [Application of AT1-angiotensin II receptor blocker valsartan in clinical practice]. Kardiologiia. 2011;51(8):77-84. Review. Russian. PubMed PMID: 21942964.

20: Bains J, Smith WB. Valsartan plus hydrochlorothiazide: a review of its use since its introduction. Expert Opin Pharmacother. 2011 Aug;12(12):1975-84. doi: 10.1517/14656566.2011.587124. Epub 2011 Jul 6. Review. PubMed PMID: 21728903.