Fimasartan - CAS 247257-48-3
Catalog number: 247257-48-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Angiotensin Receptor
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
Publictions citing BOC Sciences Products
  • >> More
> 95%
White to pale yellow powder
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
Soluble to 49mg/mL in DMSO
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).
Shelf Life:
2 years
Boiling Point:
693.0±65.0 °C | Condition: Press: 760 Torr
1.25±0.1 g/cm3
Canonical SMILES:
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∞ ( 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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Angiotensin Receptor Products

CAS 863031-24-7 Azilsartan medoxomil monopotassium

Azilsartan medoxomil monopotassium
(CAS: 863031-24-7)

Azilsartan medoxomil monopotassium is an azilsartan prodrug and and an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM. It is...

BMS 183920
(CAS: 153072-33-4)

BMS 183920, a quinoline derivative, has been found to be an angiotensin II receptor antagonist that could have potential usage in antihypertensive study.

CAS 160135-92-2 Gemopatrilat

(CAS: 160135-92-2)

Gemopatrilat, an azepan derivative, has been found to be an angiotensin receptor as well as vasopeptidase inhibitor that was once studied against hypertension a...

CAS 144689-63-4 Olmesartan Medoxomil

Olmesartan Medoxomil
(CAS: 144689-63-4)

Olmesartan Medoxomil is a compound which is hydrolyzed to olmesartan that is a selective AT1 subtype angiotensin II receptor antagonist.

CAS 133085-33-3 BIBS 39

(CAS: 133085-33-3)

BIBS 39, a nonpeptide angiotensin II receptor antagonist, has been found to exhibit potential antihypertensive activity in rat. It has been already discontinued...

CAS 145040-37-5 Candesartan Cilexetil

Candesartan Cilexetil
(CAS: 145040-37-5)

Candesartan blocks the effects of angiotensin II at the angiotensin II type 1 (AT1) receptor. Candesartan cilexetil is a prodrug that is activated to candesarta...

(CAS: 254740-64-2)

Sparsentan, also known as RE-021, BMS346567, is a dual antagonist of both angiotensin II and endothelin A receptor antagonist.

CGP 48369
(CAS: 135689-23-5)

Cgp 48369 is a nonpeptide a angiotensin type 1 receptor antagonist originated by Novartis. Treatmenf for for Hypertension in Switzerland was discontinued in 199...

CAS 863031-21-4 Azilsartan Medoxomil

Azilsartan Medoxomil
(CAS: 863031-21-4)

Azilsartan Medoxomil is a potent angiotensin II type 1 (AT1) receptor antagonist that inhibits the RAAS, with an IC50 of 2.6 nM. It exhibits more than 10,000-fo...

CAS 144701-48-4 Telmisartan

(CAS: 144701-48-4)

Telmisartan, also called Pritor, a benzimidazole derivative, is an angiotensin II receptor antagonist that can be used to treat hypertension. in vitro: activate...

PD 123177
(CAS: 114785-12-5)

PD 123177 is a Nonpeptide angiotensin type 2 receptor inhibitor. In Dec 1995, Preclinical development of it for cardiovascular disorders was began in USA.

CAS 136676-91-0 PD-123319 TFA salt

PD-123319 TFA salt
(CAS: 136676-91-0)

The ditrifluoroacetate salt form of PD-123319, a nonpeptide AT2R antagonist, could have potential effect against hypertension. It has already been discontinued ...

AVE 0991
(CAS: 304462-19-9)

AVE 0991 is an agonist of nonpeptide Ang-(1-7) receptor Mas that has potential as a cardiovascular drug.

CAS 149690-05-1 Sacubitril sodium

Sacubitril sodium
(CAS: 149690-05-1)

Sacubitril, also known as AHU377, is a first-in-class medicine that contains a neprilysin (NEP) inhibitor (sacubitril) and an angiotensin II (Ang-II) receptor b...

CAS 159432-28-7 A 779

A 779
(CAS: 159432-28-7)

A 779 is a specific antagonist of G-protein coupled receptor (Mas receptor) (IC50= 0.3 nM) with no significant affinity for AT1 or AT2 receptors at a concentrat...

CAS 144143-96-4 Eprosartan Mesylate

Eprosartan Mesylate
(CAS: 144143-96-4)

Eprosartan is a nonpeptide angiotensin II receptor antagonist, [3H]-eprosartan binds to the AT1 receptor with KD of 0.83 nM in rat vascular smooth muscle cells.

CAS 145733-36-4 Tasosartan

(CAS: 145733-36-4)

Tasosartan, a pyrido-pyrimidin derivative, has been found to be an angiotensin II receptor antagonist that could have probable effect against hypertension. It h...

CAS 147403-03-0 Azilsartan Medoxomil

Azilsartan Medoxomil
(CAS: 147403-03-0)

Azilsartan (TAK-536) is an angiotensin II receptor antagonist used in the treatment of hypertension.

CAS 70806-55-2 trans-Tranilast

(CAS: 70806-55-2)

Trans-Tranilast is an antiallergic drug used to treat bronchial asthma, allergic rhinitis and atopic dermatitis.

CAS 130663-39-7 PD123319

(CAS: 130663-39-7)

PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.

Chemical Structure

CAS 247257-48-3 Fimasartan

Quick Inquiry

Verification code

Featured Items