Shopping Cart

Your shopping cart is currently empty

Fimasartan

Name: Fimasartan
Brand: TargetMol
SKU: T2322
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

Copy Product Info

🥰Excellent

Catalog No. T2322Cas No. 247257-48-3

Alias Kanarb, BR-A-657

Fimasartan (BR-A-657) is a non-peptide angiotensin II receptor antagonist (ARB) used for the treatment of hypertension and heart failure. Concurrent administration of fimasartan with diuretic hydrochlorothiazide has shown to be safe in clinical trials.

Fimasartan

Copy Product Info

🥰Excellent

Purity: 98.96%

Catalog No. T2322Alias Kanarb, BR-A-657Cas No. 247257-48-3

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$40	In Stock	In Stock
25 mg	$62	In Stock	In Stock
50 mg	$89	In Stock	In Stock
100 mg	$139	In Stock	In Stock
200 mg	$198	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$52	In Stock	In Stock

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Batch Information

Select Batch

Purity:98.96%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Fimasartan AI Summary

Fimasartan demonstrates strong bioactivity as an antagonist at the angiotensin 2 receptor type 1, with high potency indicated by IC50 values of 0.42 nM and 0.13 nM in different assays. It shows potent antihypertensive activity in a pithed rat model with an ED50 of 0.018 mg/kg and exhibits an ED50 of 3 mg/kg with a duration of 22.0 hours for a 50% reduction in blood pressure in an angiotensin 2 induced hypertension rat model. Notably, Fimasartan also displays agonist activity at PPARgamma at 1 µM and moderate inhibitory activity against HDAC6. In terms of antiviral action, Fimasartan shows inhibition of SARS-CoV-2 3CL-Pro protease by 18.62% at 20 µM concentration but has limited efficacy against SARS-CoV-2 in various cellular assays. It inhibits cytotoxicity of Caco-2 and VERO-6 cells at 10 µM, although showing low antiviral activity in HRCE cells. Pharmacokinetics data reveal a half-life of 3.6 hours in rats at an oral dose of 10 mg/kg, with peak plasma concentrations (Cmax) of 1032.57 nM in rats and 289.04 nM in mice at the same dose. The compound's apparent permeability in MDCKII-LE cells is 1.2 x 10^-6 cm/s. It has a dissociation constant (pKa) of 4.3 and a lipophilicity (LogD) of 0.91. Additionally, Fimasartan inhibits OAT2 tv.1 by inhibiting [3H]cGMP uptake with an IC50 of 15700 nM. It also exhibits hepatic clearance rates of 23.0 and 9.6 mL.min-1.kg-1 in cynomolgus monkeys and humans, respectively. The fraction unbound in plasma is remarkably low, with values of 0.000177 and 0.000288 in cynomolgus monkeys and humans..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Fimasartan (BR-A-657) is a non-peptide angiotensin II receptor antagonist (ARB) used for the treatment of hypertension and heart failure. Concurrent administration of fimasartan with diuretic hydrochlorothiazide has shown to be safe in clinical trials.
Synonyms	Kanarb, BR-A-657

Chemical Properties

Molecular Weight	501.65
Formula	C₂₇H₃₁N₇OS
Cas No.	247257-48-3
Smiles	C(C1=CC=C(C2=C(C=CC=C2)C=3NN=NN3)C=C1)N4C(CCCC)=NC(C)=C(CC(N(C)C)=S)C4=O
Relative Density.	1.25g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (99.67 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (4.98 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9934 mL	9.9671 mL	19.9342 mL	99.6711 mL
5 mM	0.3987 mL	1.9934 mL	3.9868 mL	19.9342 mL
10 mM	0.1993 mL	0.9967 mL	1.9934 mL	9.9671 mL
20 mM	0.0997 mL	0.4984 mL	0.9967 mL	4.9836 mL
50 mM	0.0399 mL	0.1993 mL	0.3987 mL	1.9934 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc