Fasitibant chloride
Based on 1 publication(s) in Google Scholar
Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model.
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- CAS No.: 1157852-02-2
- Formula: C36H49Cl3N6O6S
- Molecular Weight:800.23
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Fasitibant chloride
MoreAll Bradykinin Receptor Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.05 nM
Compound: 4
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Displacement of [3H]bradykinin from human recombinant B2 receptor expressed in HEK293 cells
Displacement of [3H]bradykinin from human recombinant B2 receptor expressed in HEK293 cells
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[PMID: 19552431] |
Fasitibant chloride (MEN16132 free base; 1 µM; pre-treatment 30 min before BK) produces a consistent reduction of the FGF-2 expression (BK induced) and decrement of BK induced-FGFR-1 phosphorylation[2].
Fasitibant chloride inhibits the phosphorylation of FRSα, ERK1/2, STAT3 (BK induced; 1 μM; for 15 min), except AKT in HUVEC[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human umbilical vein endothelial cells (HUVEC)
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Concentration:1 µM
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Incubation Time:Pre-treatment 30 min before Bradykinin (BK; 1 μM; for 24 h)
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Result:Produced a consistent reduction of the FGF-2 expression (BK induced) and decrement of BK induced-FGFR-1 phosphorylation (without affecting FGFR-2 activity).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats weighing 250-300 g[1]
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Dosage:100 µg per knee
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Administration:Injection into the knee; 30 min before λ-carrageenan
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Result:Inhibited about 40-45% on the carrageenan-induced joint pain and knee joint oedema.
Reduced the neutrophil infiltration in the synovium by about 60% and the release of prostaglandins by about 30%.
Chemical Information
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CAS No. 1157852-02-2
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Molecular Weight 800.23
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Formula C36H49Cl3N6O6S
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SMILES
O=C(N(CC1)CCN1C([C@@H](N)CCC[N+](C)(C)C)=O)C2(CCOCC2)N[S](=O)(C(C=CC(Cl)=C3COC4=CC=CC(C(C)=C5)=C4N=C5C)=C3Cl)=O.[Cl-]
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Synonyms
MEN16132 free base
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
Endothelial Sp1/Sp3 are essential to the effect of captopril on blood pressure in male mice. [Abstract]2023 Sep 21;14(1):5891. PMID: 37735515
Purity & Documentation
References
[1]. Claudio Valenti, et al. Fasitibant Chloride, a Kinin B₂ Receptor Antagonist, and Dexamethasone Interact to Inhibit Carrageenan-Induced Inflammatory Arthritis in Rats. Br J Pharmacol. 2012 Jun;166(4):1403-10. [Content Brief]
[2]. Erika Terzuoli, et al. Bradykinin B2 Receptor Contributes to Inflammatory Responses in Human Endothelial Cells by the Transactivation of the Fibroblast Growth Factor Receptor FGFR-1. Int J Mol Sci. 2018 Sep 6;19(9):2638. [Content Brief]
[3]. Paola Cucchi, et al. MEN16132, a Novel Potent and Selective Nonpeptide Antagonist for the Human Bradykinin B2 Receptor. In Vitro Pharmacology and Molecular Characterization. Eur J Pharmacol. 2005 Dec 28;528(1-3):7-16. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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