1. GPCR/G Protein
  2. Bradykinin Receptor
  3. Fasitibant chloride

Fasitibant chloride (Synonyms: MEN16132 free base)

Cat. No.: HY-14886
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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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Fasitibant chloride Chemical Structure

Fasitibant chloride Chemical Structure

CAS No. : 1157852-02-2

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Description

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[1][2][3].

IC50 & Target
In Vitro

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].

Cell Viability Assay[2]

Cell Line: human umbilical vein endothelial cells (HUVEC)
Concentration: 1 µM
Incubation Time: Pre-treatment 30 min before Bradykinin (BK; 1 μM; for 24 h)
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).
In Vivo

Fasitibant chloride (MEN16132 free base; 100 µg per knee; injection into the knee; 30 min before λ-carrageenan) inhibits about 40-45% on the carrageenan-induced joint pain and knee joint oedema[1].

Animal Model: Male Wistar rats weighing 250-300 g[1]
Dosage: 100 µg per knee
Administration: Injection into the knee; 30 min before λ-carrageenan
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%.
Molecular Weight

800.23

Formula

C₃₆H₄₉Cl₃N₆O₆S

CAS No.

1157852-02-2

SMILES

O=C(N(CC1)CCN1C([[email protected]@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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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

FasitibantMEN16132MEN 16132MEN-16132Bradykinin ReceptornonpeptidebradykininB2receptorB2RjointpaindiminishesoedemaCarrageenanarthritisBKHUVECInhibitorinhibitorinhibit

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Fasitibant chloride
Cat. No.:
HY-14886
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