Fimasartan - CAS 247257-48-3
Catalog number: 247257-48-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C27H31N7OS
Molecular Weight:
501.66
COA:
Inquire
Targets:
Angiotensin Receptor
Description:
Fimasartan, also called as BR-A657, approved for the treatment of mild to moderate hypertension in South Korea, is a novel, non-peptide angiotensin II (Ang II) receptor antagonist with a selective type I (AT1) receptor blockade effect. Radioligand binding
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Purity:
> 95%
Appearance:
White to pale yellow powder
Synonyms:
2-[2-butyl-4-methyl-6-oxo-1-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]pyrimidin-5-yl]-N,N-dimethylethanethioamide BR-A657 fimasartan
Solubility:
Soluble to 49mg/mL in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -120℃ for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years
Quantity:
Milligrams-Grams
Boiling Point:
693.0±65.0 °C | Condition: Press: 760 Torr
Density:
1.25±0.1 g/cm3
InChIKey:
AMEROGPZOLAFBN-UHFFFAOYSA-N
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)
Canonical SMILES:
CCCCC1=NC(=C(C(=O)N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)CC(=S)N(C)C)C
1.Population Pharmacokinetic Modeling of the Enterohepatic Recirculation of Fimasartan in Rats, Dogs, and Humans.
Kim TH1, Shin S, Landersdorfer CB, Chi YH, Paik SH, Myung J, Yadav R, Horkovics-Kovats S, Bulitta JB, Shin BS. AAPS J. 2015 Sep;17(5):1210-23. doi: 10.1208/s12248-015-9764-2. Epub 2015 May 20.
Enterohepatic recirculation (EHC) can greatly enhance plasma drug exposures and therapeutic effects. This study aimed to develop a population pharmacokinetic model that can simultaneously characterize the extent and time-course of EHC in three species using fimasartan, a novel angiotensin II receptor blocker, as a model drug. All fimasartan plasma concentration profiles in 32 rats (intravenous doses, 0.3-3 mg/kg; oral doses, 1-10 mg/kg), 34 dogs (intravenous doses, 0.3-1 mg/kg; oral doses, 1-10 mg/kg), and 42 healthy volunteers (single or multiple oral doses, 20-480 mg) were determined via liquid chromatography-tandem mass spectrometry (LC-MS/MS) and simultaneously modeled in S-ADAPT. The proposed model quantitatively characterized EHC in three species after oral and intravenous dosing. The median (range) fraction of drug undergoing recirculation was 76.3% (64.9-88.7%) in rats, 33.3% (24.0-45.9%) in dogs, and 65.6% (56.5-72.0%) in humans.
2.Absolute bioavailability and pharmacokinetics of the angiotensin II receptor antagonist fimasartan in healthy subjects.
Ghim JL1, Paik SH2, Hasanuzzaman M3, Chi YH2, Choi HK3, Kim DH3, Shin JG1,3. J Clin Pharmacol. 2015 Aug 13. doi: 10.1002/jcph.618. [Epub ahead of print]
The present study was conducted to determine the absolute bioavailability of fimasartan (FMS; Kanarb®) after the single oral administration of a 60-mg tablet or a single 30-mg intravenous (IV) infusion. This investigation was a randomized, single-dose, open-labeled, two-way crossover study of 16 healthy Korean male subjects. The subjects were divided into two groups (n = 8) and each received either the oral or IV formulation followed by one-week washout period. The Cmax (ng/ml) and AUC∞ (h.ng/ml) following oral and IV administration were 62.39 ± 48.62 and 291.12 ± 121.65; and 683.26 ± 104.30 and 782.27 ± 112.71 (mean ± SD), respectively. The Tmax (h) were 3.00 h (range: 0.50-5.00 h) and 1.00 h (range: 0.75-1.00 h) in the test and reference groups, respectively. The terminal elimination half-lives (t1/2, h) were similar (5.77 and 5.51 h, respectively) indicating that the route of administration did not influence the absorption or elimination of FMS.
3.Telmisartan attenuates hyperglycemia-exacerbated VCAM-1 expression and monocytes adhesion in TNFα-stimulated endothelial cells by inhibiting IKKβ expression.
Song KH1, Park JH2, Jo I2, Park JY3, Seo J4, Kim SA5, Cho DH6. Vascul Pharmacol. 2016 Mar;78:43-52. doi: 10.1016/j.vph.2015.10.001. Epub 2015 Oct 8.
Uncontrolled hyperglycemia accelerates endothelial damage and vascular inflammation caused by proinflammatory cytokines including tumor necrosis factor α (TNFα), which leads to arteriosclerotic cardiovascular diseases such as myocardial infarction. Telmisartan, an angiotensin II type 1 receptor blocker (ARB), is prescribed for treatment of hypertensive patients with concurrent diabetes mellitus (DM). Although a few clinical trials have suggested that telmisartan decreases cardiovascular complications in diabetic patients, the molecular mechanism for the beneficial effects remains elusive. Here, we investigated a molecular mechanism and effects of telmisartan on the expression of vascular cell adhesion molecule-1 (VCAM-1) and attachment of monocytes onto endothelial cells induced by TNFα in hyperglycemia-treated bovine aortic endothelial cells (BAEC). Telmisartan dose-dependently decreased hyperglycemia-aggravated IκB kinase β (IKKβ) expression and nuclear factor-κB (NF-κB) p65-Ser(536) phosphorylation, which accompanied a decrease in VCAM-1 expression and THP-1 monocytes adhesion.
4.Anti-inflammatory effects of fimasartan via Akt, ERK, and NFκB pathways on astrocytes stimulated by hemolysate.
Yang XL1,2, Kim CK1,2,3, Kim TJ1,2, Sun J2, Rim D1, Kim YJ1,2, Ko SB1,2, Jang H1,2, Yoon BW4,5,6. Inflamm Res. 2016 Feb;65(2):115-23. doi: 10.1007/s00011-015-0895-9. Epub 2015 Nov 25.
OBJECTIVE: The aim of this study was to investigate whether fimasartan, a novel angiotensin II receptor blocker, modulates hemolysate-induced inflammation in astrocytes.
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CAS 247257-48-3 Fimasartan

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