Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fasitibant chloride (MEN16132 free base) is a powerful and specific nonpeptide antagonist of the bradykinin B2 receptor (B2R). This compound effectively reduces joint pain and mitigates joint edema in a rat model of Carrageenan-induced arthritis.
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25 mg | Inquiry | $ 1,520.00 |
Description | Fasitibant chloride (MEN16132 free base) is a powerful and specific nonpeptide antagonist of the bradykinin B2 receptor (B2R). This compound effectively reduces joint pain and mitigates joint edema in a rat model of Carrageenan-induced arthritis. |
In vitro | Fasitibant chloride (MEN16132 free base; 1 μM; pre-treatment 30 min before BK) consistently reduces FGF-2 expression and decreases BK-induced FGFR-1 phosphorylation without affecting FGFR-2 activity. Additionally, it impedes the phosphorylation of FRSα, ERK1/2, and STAT3, excluding AKT, in HUVEC. In a cell viability assay on human umbilical vein endothelial cells (HUVEC) with a concentration of 1 μM and pre-treatment 30 min before exposure to Bradykinin (BK; 1 μM; for 24 h), fasitibant chloride demonstrated a similar reduction in FGF-2 expression and decrease in BK-induced FGFR-1 phosphorylation. |
In vivo | Fasitibant chloride (MEN16132 free base; 100 μg per knee; injected into the knee 30 minutes before λ-carrageenan) effectively reduces carrageenan-induced joint pain and knee joint edema by 40-45% in male Wistar rats weighing 250-300 g[1]. The treatment also significantly decreases neutrophil infiltration in the synovium by approximately 60% and prostaglandin release by around 30%, showcasing its potent anti-inflammatory and analgesic properties. |
Synonyms | MEN16132 free base, Fasitibant chloride |
Molecular Weight | 800.23 |
Formula | C36H49Cl3N6O6S |
CAS No. | 1157852-02-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Fasitibant chloride 1157852-02-2 MEN 16132 MEN16132 free base MEN16132 Fasitibant Chloride MEN-16132 inhibitor inhibit