Home GPCR & G Protein Angiotensin Receptor antagonist Fimasartan For research use only.

Fimasartan

Synonyms: Kanarb

Fimasartan (Kanarb) is a non-peptide angiotensin II receptor antagonist (ARB) with noncompetitive, insurmountable binding with the AT1 receptor. It is used for the treatment of hypertension and heart failure.

Fimasartan Chemical Structure

Fimasartan Chemical Structure

CAS No. 247257-48-3

Purity & Quality Control

Batch: S497501 DMSO]100 mg/mL]false]Ethanol]24 mg/mL]false]Water]Insoluble]false Purity: 99.75%
99.75

Fimasartan Related Products

Biological Activity

Description Fimasartan (Kanarb) is a non-peptide angiotensin II receptor antagonist (ARB) with noncompetitive, insurmountable binding with the AT1 receptor. It is used for the treatment of hypertension and heart failure.
Targets
AT1 receptor [1]
In vitro
In vitro

Fimasartan is a selective AT1 receptor antagonist. The concentration that inhibits the binding of [125I]Ang II to the AT1 receptor from rat adrenal cortex by 50% (IC50) is 0.13 nM. Fimasartan potently attenuates myocardial apoptotic death in reperfused rat heart and H9c2 cells. Fimasartan could attenuate mitochondrial damage which is associated with minimizing the reduction in Bcl-2 and connected with the reduction in p53 and activation of Akt and GSK-3β, and inhibiting mitochondrial Ca2+ overload by suppressing the ICa,L and MCU[2].
Cell Research Cell lines H9c2 cells
Concentrations 50 μM
Incubation Time 24 h
Method

H9c2 cells are pretreated with fimasartan (50 μM) for 24 h prior to experiencing 18-h/48-h reoxygenation.
In Vivo
In vivo

In various animal models including renal hypertensive rats, spontaneously hypertensive rats and Beagle dogs, fimasartan effectively reduces blood pressure in a dose-dependent manner following single or repeated oral and intravenous administration. Fimasartan does not affect general behavior, respiratory rate or tidal volume in experimental animals, and shows no adverse findings in the human ether-a-go-go-related gene (hERG) test or monkey telemetry study. A number of general toxicity, carcinogenic toxicity, genetic toxicity, and developmental toxicity studies given either orally or intravenously in various species including mice, rats, monkeys and dogs are conducted and these preclinical results demonstrate the safety and tolerability of fimasartan for long-term clinical use and offer sufficient safety margins to support the expected human therapeutic dose. Fimasartan is rapidly absorbed following oral administration with the time to peak plasma concentration (Tmax) ranging 0.5-3 h and the terminal half-life (t1/2) being 5-16 h at doses of 20 to 480 mg in healthy subjects. Similar results are obtained in patients with hypertension, i.e., Tmax ranges 0.5-1.3 h and t1/2 is 7-10 h following fimasartan administration at doses 20-180 mg in the subsequent phase II study. The urinary excretion of fimasartan is low, with the overall urinary excretion of unchanged drug over the first 24 h after dosing being less than 3% of the administered dose. Fimasartan undergoes nonrenal elimination with minimal metabolism[1]. Fimasartan treatment before myocardial ischemia significantly attenuates reperfusion injury and apoptotic changes, possibly by suppressing mitochondrial damage during reperfusion[2]. In various preclinical studies, including aortic balloon injury, myocardial infarct ischemia/reperfusion, doxorubicin cardiotoxicity, and ischemic stroke models, fimasartan shows anti-inflammatory and organ-protecting effects[3].
Animal Research Animal Models Sprague-Dawley rats (animal model with myocardial ischemia/reperfusion injury)
Dosages 3 mg/kg
Administration i.v
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02994745 Completed
Hypertension Hyperlipidemia
Boryung Pharmaceutical Co. Ltd
 December 23 2016 Phase 1
NCT02920047 Completed
Hypertension
Boryung Pharmaceutical Co. Ltd
 October 2016 Phase 1
NCT02995720 Completed
Hypertension Hyperlipidemia
Boryung Pharmaceutical Co. Ltd
 August 26 2016 Phase 1
NCT03231293 Completed
Hypertension|Ischemic Stroke|Transient Ischemic Attack
Boryung Pharmaceutical Co. Ltd
 July 28 2016 --

Chemical Information & Solubility

Molecular Weight 501.65 Formula

C27H31N7OS
CAS No. 247257-48-3 SDF --
Smiles CCCCC1=NC(=C(C(=O)N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)CC(=S)N(C)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (199.34 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 24 mg/mL

Water : Insoluble


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In vivo
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