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Fasitibant chloride (MEN16132 free base) is a potent and specific nonpeptide antagonist of the bradykinin B2 receptor (B2R), effectively reducing joint pain and mitigating joint edema in a rat model of Carrageenan-induced arthritis.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | Inquiry | Inquiry |
| Description | Fasitibant chloride (MEN16132 free base) is a potent and specific nonpeptide antagonist of the bradykinin B2 receptor (B2R), effectively reducing joint pain and mitigating 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 diminishes BK-induced FGFR-1 phosphorylation without affecting FGFR-2 activity in HUVECs, also impeding the phosphorylation of FRSα, ERK1/2, and STAT3 but not AKT. In a cell viability assay on HUVECs, it demonstrated the same 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 potent anti-inflammatory and analgesic properties. |
| Synonyms | MEN16132 free base, Fasitibant chloride |
| Molecular Weight | 800.23 |
| Formula | C36H49Cl3N6O6S |
| Cas No. | 1157852-02-2 |
| Smiles | [Cl-].Cc1cc(C)c2cccc(OCc3c(Cl)ccc(c3Cl)S(=O)(=O)NC3(CCOCC3)C(=O)N3CCN(CC3)C(=O)[C@@H](N)CCC[N+](C)(C)C)c2n1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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