Fimasartan
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MedKoo CAT#: 317141

CAS#: 247257-48-3 (free)

Description: Fimasartan is a non-peptide angiotensin II receptor antagonist (ARB) used for the treatment of hypertension and heart failure. Through oral administration, fimasartan blocks angiotensin II receptor type 1 (AT1 receptors), reducing pro-hypertensive actions of angiotensin II, such as systemic vasoconstriction and water retention by the kidneys. Fimasartan was approved for use in South Korea in September 9th, 2010.


Chemical Structure

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Fimasartan
CAS# 247257-48-3 (free)

Theoretical Analysis

MedKoo Cat#: 317141
Name: Fimasartan
CAS#: 247257-48-3 (free)
Chemical Formula: C27H31N7OS
Exact Mass: 501.23108
Molecular Weight: 501.65
Elemental Analysis: C, 64.65; H, 6.23; N, 19.55; O, 3.19; S, 6.39

Size Price Shipping out time Quantity
100mg USD 150 2 Weeks
200mg USD 250 2 Weeks
500mg USD 450 2 Weeks
1g USD 750 2 Weeks
2g USD 1250 2 Weeks
5g USD 2250 2 Weeks
10g USD 3850 2 Weeks
20g USD 5850 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-01. Prices are subject to change without notice.

Fimasartan, purity > 98%, is in stock. The same day shipping out after order is received.

Related CAS #: 1020110-23-9 (potassium trihydrate)   247257-48-3 (free)   1402813-38-0 (potassium)    

Synonym: BR-A657; BR A657; BRA657; BRA 657; BR-A-657.K; Fimasartan. brand name: Kanarb.

IUPAC/Chemical Name: 2-(2-Butyl-4-methyl-6-oxo-1-{[2'-(1H-tetrazol-5-yl)-4-biphenylyl]methyl}-1,6-dihydro-5-pyrimidinyl)-N,N-dimethylethanethioamide

InChi Key: AMEROGPZOLAFBN-UHFFFAOYSA-N

InChi Code: InChI=1S/C27H31N7OS/c1-5-6-11-24-28-18(2)23(16-25(36)33(3)4)27(35)34(24)17-19-12-14-20(15-13-19)21-9-7-8-10-22(21)26-29-31-32-30-26/h7-10,12-15H,5-6,11,16-17H2,1-4H3,(H,29,30,31,32)

SMILES Code: S=C(N(C)C)CC1=C(C)N=C(CCCC)N(CC2=CC=C(C3=CC=CC=C3C4=NN=NN4)C=C2)C1=O

Appearance:
Solid 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

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 501.65 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.

Select a batch to recalculate based on the batch molecular weight:
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

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1: Kim CK, Yang XL, Kim YJ, Choi IY, Jeong HG, Park HK, Kim D, Kim TJ, Jang H, Ko SB, Yoon BW. Effect of Long-Term Treatment with Fimasartan on Transient Focal Ischemia in Rat Brain. Biomed Res Int. 2015;2015:295925. doi: 10.1155/2015/295925. Epub 2015 Sep 13. PubMed PMID: 26448932; PubMed Central PMCID: PMC4584036.

2: Ghim JL, Paik SH, Hasanuzzaman M, Chi YH, Choi HK, Kim DH, Shin JG. Absolute bioavailability and pharmacokinetics of the angiotensin II receptor antagonist fimasartan in healthy subjects. J Clin Pharmacol. 2015 Aug 13. doi: 10.1002/jcph.618. [Epub ahead of print] PubMed PMID: 26272450.

3: Rhee MY, Baek SH, Kim W, Park CG, Park SW, Oh BH, Kim SH, Kim JJ, Shin JH, Yoo BS, Rim SJ, Ha JW, Doh JH, Ahn Y, Chae JK, Park JB, Kim SK, Kim CH. Efficacy of fimasartan/hydrochlorothiazide combination in hypertensive patients inadequately controlled by fimasartan monotherapy. Drug Des Devel Ther. 2015 Jun 2;9:2847-54. doi: 10.2147/DDDT.S82098. eCollection 2015. PubMed PMID: 26082615; PubMed Central PMCID: PMC4459623.

4: Lee JY, Choi YJ, Oh SJ, Chi YH, Paik SH, Lee KH, Jung JK, Ryu CS, Kim KB, Kim DH, Yoon YR, Kim SK. Characterization of fimasartan metabolites in human liver microsomes and human plasma. Xenobiotica. 2015 Jun 11:1-12. [Epub ahead of print] PubMed PMID: 26068523.

5: Kim TH, Shin S, Landersdorfer CB, Chi YH, Paik SH, Myung J, Yadav R, Horkovics-Kovats S, Bulitta JB, Shin BS. Population Pharmacokinetic Modeling of the Enterohepatic Recirculation of Fimasartan in Rats, Dogs, and Humans. AAPS J. 2015 Sep;17(5):1210-23. doi: 10.1208/s12248-015-9764-2. Epub 2015 May 20. PubMed PMID: 25990964; PubMed Central PMCID: PMC4540730.

6: Chang SA, Lim BK, Lee YJ, Hong MK, Choi JO, Jeon ES. A Novel Angiotensin Type I Receptor Antagonist, Fimasartan, Prevents Doxorubicin-induced Cardiotoxicity in Rats. J Korean Med Sci. 2015 May;30(5):559-68. doi: 10.3346/jkms.2015.30.5.559. Epub 2015 Apr 15. PubMed PMID: 25931786; PubMed Central PMCID: PMC4414639.

7: Lee HY, Kim YJ, Ahn T, Youn HJ, Chull Chae S, Seog Seo H, Kim KS, Rhee MY, Choi DJ, Kim JJ, Chun KJ, Yoo BS, Park JS, Oh SK, Kim DS, Kwan J, Ahn Y, Bae Park J, Jeong JO, Hyon MS, Cho EJ, Han KR, Kim DI, Joo SJ, Shin JH, Sung KC, Jeon ES. A Randomized, Multicenter, Double-Blind, Placebo-Controlled, 3 × 3 Factorial Design, Phase II Study to Evaluate the Efficacy and Safety of the Combination of Fimasartan/Amlodipine in Patients With Essential Hypertension. Clin Ther. 2015 Apr 4. pii: S0149-2918(15)00089-2. doi: 10.1016/j.clinthera.2015.02.019. [Epub ahead of print] PubMed PMID: 25850881.

8: Yoon SH, Oh S, Kim HS, Yi S, Yu KS, Jang IJ, Cho JY. Validated LC-MS/MS Assay for the Quantitative Determination of Fimasartan in Human Plasma: Application to Pharmacokinetic Studies. J Chromatogr Sci. 2015 Sep;53(8):1250-6. doi: 10.1093/chromsci/bmu219. Epub 2015 Jan 22. PubMed PMID: 25616988.

9: Sim DS, Jeong MH, Song HC, Kim J, Chong A, Bom HS, Jeong IS, Oh SG, Kim JM, Park DS, Kim JH, Lim KS, Kim MS, Ryu SH, Kim HK, Kim SS, Jang SY, Cho JY, Jeong HC, Lee KH, Park KH, Yoon NS, Yoon HJ, Kim KH, Hong YJ, Park HW, Kim JH, Ahn Y, Cho JG, Park JC, Kang JC. Cardioprotective effect of fimasartan, a new angiotensin receptor blocker, in a porcine model of acute myocardial infarction. J Korean Med Sci. 2015 Jan;30(1):34-43. doi: 10.3346/jkms.2015.30.1.34. Epub 2014 Dec 23. PubMed PMID: 25552881; PubMed Central PMCID: PMC4278025.

10: Kim S, Lee J, Shin D, Lim KS, Kim YS, Jang IJ, Yu KS. Effect of renal function on the pharmacokinetics of fimasartan: a single-dose, open-label, Phase I study. Drug Des Devel Ther. 2014 Oct 6;8:1723-31. doi: 10.2147/DDDT.S68784. eCollection 2014. PubMed PMID: 25336916; PubMed Central PMCID: PMC4199969.

11: Youn JC, Ihm SH, Bae JH, Park SM, Jeon DW, Jung BC, Park TH, Lee NH, Song JM, Yoon YW, Shin ES, Sung KC, Jung IH, Pyun WB, Joo SJ, Park WJ, Shin JH, Kang SM. Efficacy and safety of 30-mg fimasartan for the treatment of patients with mild to moderate hypertension: an 8-week, multicenter, randomized, double-blind, phase III clinical study. Clin Ther. 2014 Oct 1;36(10):1412-21. doi: 10.1016/j.clinthera.2014.07.004. Epub 2014 Aug 3. PubMed PMID: 25092393.

12: Jeong ES, Kim YW, Kim HJ, Shin HJ, Shin JG, Kim KH, Chi YH, Paik SH, Kim DH. Glucuronidation of fimasartan, a new angiotensin receptor antagonist, is mainly mediated by UGT1A3. Xenobiotica. 2015 Jan;45(1):10-8. doi: 10.3109/00498254.2014.942810. Epub 2014 Jul 18. PubMed PMID: 25034008.

13: Kim TH, Shin S, Bashir M, Chi YH, Paik SH, Lee JH, Choi HJ, Choi JH, Yoo SD, Bulitta JB, Ma E, Joo SH, Shin BS. Pharmacokinetics and metabolite profiling of fimasartan, a novel antihypertensive agent, in rats. Xenobiotica. 2014 Oct;44(10):913-25. doi: 10.3109/00498254.2014.915359. Epub 2014 Apr 30. PubMed PMID: 24786684.

14: Kim CO, Lee HW, Oh ES, Seong SJ, Kim do Y, Lee J, Ahn SH, Yoon YR, Cho CM, Park MS. Influence of hepatic dysfunction on the pharmacokinetics and safety of fimasartan. J Cardiovasc Pharmacol. 2013 Dec;62(6):524-9. doi: 10.1097/FJC.0000000000000010. PubMed PMID: 24084213.

15: Lee H, Kim KS, Chae SC, Jeong MH, Kim DS, Oh BH. Ambulatory blood pressure response to once-daily fimasartan: an 8-week, multicenter, randomized, double-blind, active-comparator, parallel-group study in Korean patients with mild to moderate essential hypertension. Clin Ther. 2013 Sep;35(9):1337-49. doi: 10.1016/j.clinthera.2013.06.021. Epub 2013 Aug 7. PubMed PMID: 23932463.

16: Han J, Park SJ, Thu VT, Lee SR, Long le T, Kim HK, Kim N, Park SW, Jeon ES, Kim EJ, Yoon CH, Cho GY, Choi DJ. Effects of the novel angiotensin II receptor type I antagonist, fimasartan on myocardial ischemia/reperfusion injury. Int J Cardiol. 2013 Oct 3;168(3):2851-9. doi: 10.1016/j.ijcard.2013.03.151. Epub 2013 May 1. PubMed PMID: 23642815.

17: Lee JY, Lee CW, Kim WJ, Ahn JM, Park DW, Kang SJ, Lee SW, Kim YH, Son WC, Jung S, Park SW, Park SJ. Antiatherosclerotic effects of the novel angiotensin receptor antagonist Fimasartan on plaque progression and stability in a rabbit model: a double-blind placebo-controlled trial. J Cardiovasc Pharmacol. 2013 Aug;62(2):229-36. doi: 10.1097/FJC.0b013e318297458b. PubMed PMID: 23615162.

18: Ryu S, Shin JS, Cho YW, Kim HK, Paik SH, Lee JH, Chi YH, Kim JH, Kim JH, Lee KT. Fimasartan, anti-hypertension drug, suppressed inducible nitric oxide synthase expressions via nuclear factor-kappa B and activator protein-1 inactivation. Biol Pharm Bull. 2013;36(3):467-74. PubMed PMID: 23449332.

19: Lim HJ, Lee SK, Lim DY. Influence of Fimasartan (a Novel AT(1) Receptor Blocker) on Catecholamine Release in the Adrenal Medulla of Spontaneously Hypertensive Rats. Korean J Physiol Pharmacol. 2013 Feb;17(1):99-109. doi: 10.4196/kjpp.2013.17.1.99. Epub 2013 Feb 14. PubMed PMID: 23441003; PubMed Central PMCID: PMC3579112.

20: Kim JW, Yi S, Kim TE, Lim KS, Yoon SH, Cho JY, Lee MG, Song IS, Shin SG, Jang IJ, Yu KS. Increased systemic exposure of fimasartan, an angiotensin II receptor antagonist, by ketoconazole and rifampicin. J Clin Pharmacol. 2013 Jan;53(1):75-81. doi: 10.1177/0091270011433328. Epub 2013 Jan 24. PubMed PMID: 23400746.