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: 247257-48-3

Selleck's Fimasartan has been cited by 1 publication

Purity & Quality Control

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

Related compound libraries

Choose Selective Angiotensin Receptor Inhibitors

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 shows superior inhibitory activity in the contraction of isolated rabbit thoracic aorta compared to other ARBs such as losartan and candesartan[1]. 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 lnformation & 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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Fimasartan | Fimasartan supplier | purchase Fimasartan | Fimasartan cost | Fimasartan manufacturer | order Fimasartan | Fimasartan distributor