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Fasitibant chloride

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Catalog No. T38544Cas No. 1157852-02-2
Alias MEN16132 free base, Fasitibant chloride

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.

Fasitibant chloride

Fasitibant chloride

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Catalog No. T38544Alias MEN16132 free base, Fasitibant chlorideCas No. 1157852-02-2
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.
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
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.
SynonymsMEN16132 free base, Fasitibant chloride
Chemical Properties
Molecular Weight800.23
FormulaC36H49Cl3N6O6S
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 & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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