Art. -Nr.: HY-B0780

Fimasartan

(Synonyms: BR-A-657)

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

Fimasartan (BRA-657) is an orally effective angiotensin receptor AT1 non-peptide antagonist. Fimasartan has antihypertensive effects. Fimasartan improves neuroinflammation and brain injury mediated by NLRP3 inflammatome after intracerebral hemorrhage, and has neuroprotective effect. Fimasartan inhibits the expression of inducible nitric oxide synthase through the inactivation of NF-κB and activator protein-1.

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Reinheit: 99.60%
CAS. Nr.: 247257-48-3
Formel: C₂₇H₃₁N₇OS
Molecular Weight:501.65

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Fimasartan Chemical Structure

CAS. Nr.: 247257-48-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

AT1 Receptor

Alle Angiotensin Receptor Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

In Vitro

Fimasartan (62.5, 125 and 250 µM; 1 h) inhibits NO production and the expression of inducible nitric oxide synthase in LPS(HY-D1056)-induced RAW264.7 macrophages^[1].
Fimasartan (250 µM; 1 h) decreases the activation of NF-κB and activator protein 1 in LPS(HY-D1056)-induced RAW264.7 macrophages^[1].
Fimasartan (30 ng/mL; 6 h) inhibits the activation of the NLRP3 inflammatome in a hemolysate -induced microglia model simulating cerebral hemorrhage^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

LPS treated RAW264.7 macrophages
Concentration:

62.5, 125 and 250µM
Incubation Time:

1 h
Result:

Reduced the levels of inducible nitric oxide synthase in a concentration‐dependent manner.

Western Blot Analysis^[2]

Cell Line:

BV2 microglia cell
Concentration:

30 ng/mL
Incubation Time:

6 h
Result:

Reduced the levels of NLRPS, ASC and cleaved caspase-1.

In Vivo

Fimasartan (0.5 mg/kg; Oral administration; 33 days) ameliorates NLRP3 inflammasome-mediated neuroinflammation and brain injury in a rat model of cerebral hemorrhage^[2].
Fimasartan (0.03-3 mg/kg; Oral administration/Intravenous injection; 3-24 h) has antihypertensive effect in hypertensive rats^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Intracerebral hemorrhage treated male Sprague-Dawley rats aged four weeks old (65-75 g)^[2]
Dosage:

Low-dose (0.5 mg/kg); regular-doses (1.0 and 3.0 mg/kg)
Administration:

Oral administration (p.o.); 33 days
Result:

Reduced blood pressure in a dose-dependent manner in the regular-dose groups, the blood pressure in the low-dose groups was not significantly different from that of control groups.
Attenuated intracerebral hemorrhage-induced edema and improved neurological functions in the regular-dose groups.
Significantly decreased the activation of NLRP3/ASC/caspase-1 and NF-κB pathways after intracerebral hemorrhage in the regular-dose groups.

Animal Model:

Male Sprague-Dawley rats (280-320g)^[3]
Dosage:

0.03, 0.1, 0.3mg/kg;
1, 3 mg/kg
Administration:

Intravenous injection (i.v.); 3 h;
Oral administration (p.o.); 24 h
Result:

Significantly decreased in mean arterial blood pressure with rapid onset a dose-dependent manner by i.v. and p.o.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 247257-48-3
Appearance Solid
Molecular Weight 501.65
Formel C₂₇H₃₁N₇OS
Color Off-white to light yellow
SMILES

O=C1N(C(CCCC)=NC(C)=C1CC(N(C)C)=S)CC2=CC=C(C3=C(C4=NN=NN4)C=CC=C3)C=C2
Synonyms

BR-A-657
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Journal Impact Factor

Cancer Cell Int

Antiproliferative and apoptotic effects of telmisartan in human glioma cells. [Abstract]

2023 Jun 9;23(1):111. PMID: 37291545
J Pharm Sci

Prediction of the Time to Reach Equilibrium for Improved Estimation of the Unbound Fraction of Compounds in Equilibrium Dialysis using Kinetic Modeling. [Abstract]

2023 Nov;112(11):2901-2909. PMID: 37392902
Immunopathol Persa

2025 Sep 20:e43864
J Med Life

Fimasartan ameliorates renal ischemia reperfusion injury via modulation of oxidative stress, inflammatory and apoptotic cascades in a rat model. [Abstract]

2022 Feb;15(2):241-251. PMID: 35419091

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (199.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9934 mL

9.9671 mL

19.9342 mL

5 mM

0.3987 mL

1.9934 mL

3.9868 mL

10 mM

0.1993 mL

0.9967 mL

1.9934 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ryu S, et al. Fimasartan, anti-hypertension drug, suppressed inducible nitric oxide synthase expressions via nuclear factor-kappa B and activator protein-1 inactivation. Biol Pharm Bull. 2013;36(3):467-74. [Content Brief]

[2]. Yang X, Sun J, Kim TJ, Kim YJ, Ko SB, Kim CK, Jia X, Yoon BW. Pretreatment with low-dose fimasartan ameliorates NLRP3 inflammasome-mediated neuroinflammation and brain injury after intracerebral hemorrhage. Exp Neurol. 2018 Dec;310:22-32. [Content Brief]

[3]. Chi YH, et al. Pharmacological characterization of BR-A-657, a highly potent nonpeptide angiotensin II receptor antagonist. Biol Pharm Bull. 2013;36(7):1208-15. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9934 mL	9.9671 mL	19.9342 mL	49.8355 mL
	5 mM	0.3987 mL	1.9934 mL	3.9868 mL	9.9671 mL
	10 mM	0.1993 mL	0.9967 mL	1.9934 mL	4.9836 mL
	15 mM	0.1329 mL	0.6645 mL	1.3289 mL	3.3224 mL
	20 mM	0.0997 mL	0.4984 mL	0.9967 mL	2.4918 mL
	25 mM	0.0797 mL	0.3987 mL	0.7974 mL	1.9934 mL
	30 mM	0.0664 mL	0.3322 mL	0.6645 mL	1.6612 mL
	40 mM	0.0498 mL	0.2492 mL	0.4984 mL	1.2459 mL
	50 mM	0.0399 mL	0.1993 mL	0.3987 mL	0.9967 mL
	60 mM	0.0332 mL	0.1661 mL	0.3322 mL	0.8306 mL
	80 mM	0.0249 mL	0.1246 mL	0.2492 mL	0.6229 mL
	100 mM	0.0199 mL	0.0997 mL	0.1993 mL	0.4984 mL

Keywords

Fimasartan

4 Cited Publications

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Fimasartan

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Publications Citing Use of MedChemExpress (MCE) Fimasartan

Alle Angiotensin Receptor Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Fimasartan Related Classifications

HY-B0780 Related Classifications