2. GPCR/G Protein Apoptosis
  3. Angiotensin Receptor Apoptosis
  4. Fimasartan

Fimasartan  (Synonyms: BR-A-657)

Cat. No.: HY-B0780 Purity: 98.55%
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Fimasartan(BR-A-657) is a non-peptide angiotensin II receptor antagonist used for the treatment of hypertension and heart failure.

For research use only. We do not sell to patients.

Fimasartan Chemical Structure

Fimasartan Chemical Structure

CAS No. : 247257-48-3

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Based on 4 publication(s) in Google Scholar

Other Forms of Fimasartan:

Fimasartan Related Antibodies

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AT1 Receptor AT2 Receptor

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Description

Fimasartan(BR-A-657) is a non-peptide angiotensin II receptor antagonist used for the treatment of hypertension and heart failure. IC50 value: Target: AT1 receptor antagonist in vitro: Fimasartan suppressed the expressions of inducible nitric oxide synthase (iNOS) by down-regulating its transcription, and subsequently inhibited the productions of nitric oxide (NO). In addition, fimasartan attenuated LPS-induced transcriptional and DNA-binding activities of nuclear factor-kappa B (NF-κB) and activator protein-1 (AP-1) [1]. BR-A-657 displaced [125I][Sar1 -Ile8]angiotensin II (Ang II) from its specific binding sites to AT1 subtype receptors in membrane fractions of HEK-293 cells with an IC50 of 0.16 nM [2]. in vivo: After oral administration of 240 mg fimasartan, the mean area under the plasma concentration-time curve from time zero to infinity was 2899.0 ng/ml/h in the older, which was significantly greater than in young subjects (1767.4 ng/ml/h; p = 0.03) [3]. Compared with atorvastatin alone, coadministration of fimasartan and atorvastatin increased the atorvastatin acid mean (95% confidence interval) maximum concentration (Cmax,ss) by 1.89-fold (1.49-2.39) and the area under the concentration curve (AUCτ,ss) by 1.19-fold (0.96-1.48). Fimasartan also increased the mean 2-hydroxy atorvastatin acid Cmax,ss and AUCτ,ss by 2.45-fold (1.80-3.35) and 1.42-fold (1.09-1.85), respectively [4].

IC50 & Target

AT1 Receptor

 

Clinical Trial
Molecular Weight

501.65

Formula

C27H31N7OS
CAS No.
Appearance

Solid

Color

Light yellow to 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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 49 mg/mL (97.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9934 mL 9.9671 mL 19.9342 mL
5 mM 0.3987 mL 1.9934 mL 3.9868 mL
View the Complete Stock Solution Preparation Table

* 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.

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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Fimasartan Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fimasartan247257-48-3BR-A-657Angiotensin ReceptorApoptosisInhibitorinhibitorinhibit

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