1157852-02-2
1157852-02-2 structure
- Name: Fasitibant chloride
- Chemical Name: [(4S)-4-amino-5-[4-[4-[[2,4-dichloro-3-[(2,4-dimethylquinolin-8-yl)oxymethyl]phenyl]sulfonylamino]oxane-4-carbonyl]piperazin-1-yl]-5-oxopentyl]-trimethylazanium
- CAS Number: 1157852-02-2
- Molecular Formula: C36H49Cl3N6O6S
- Molecular Weight: 764.78200
- Catalog: Signaling Pathways GPCR/G Protein Bradykinin Receptor
- Create Date: 2017-11-06 15:25:28
- Modify Date: 2024-01-07 16:34:45
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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[1][2][3].
| Name | [(4S)-4-amino-5-[4-[4-[[2,4-dichloro-3-[(2,4-dimethylquinolin-8-yl)oxymethyl]phenyl]sulfonylamino]oxane-4-carbonyl]piperazin-1-yl]-5-oxopentyl]-trimethylazanium |
|---|---|
| Synonyms |
Fasitibant chloride
UNII-0WL827Z7AE Fasitibant UNII-7J764K70IG |
| 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]. |
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| Related Catalog | |
| Target |
B2R[1][2] |
| 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%. |
| References |
| Molecular Formula | C36H49Cl3N6O6S |
|---|---|
| Molecular Weight | 764.78200 |
| Exact Mass | 763.28100 |
| PSA | 152.54000 |
| LogP | 6.09720 |