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

Fimasartan  (Synonyms: BR-A-657)

Cat. No.: HY-B0780 Purity: 98.55%
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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.

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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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 66 In-stock
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10 mM * 1 mL in DMSO USD 66 In-stock
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Based on 4 publication(s) in Google Scholar

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Fimasartan Related Antibodies

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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Description

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[1][2][3].

IC50 & Target

AT1 Receptor

 

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.

Fimasartan Related Antibodies

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
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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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 ReceptorApoptosisNF-κBNuclear factor-κBNuclear factor-kappaBAntihypertensive agentAT1RAW264.7 macrophagesBV2 microglia cellCerebral hemorrhage modelHypertension modelInhibitorinhibitorinhibit

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