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.
Product information
CAS Number: 1157852-02-2
Molecular Weight: 800.23
Formula: C36H49Cl3N6O6S
Chemical Name: (4-amino-5-{4-[4-(2,4-dichloro-3-{[(2,4-dimethylquinolin-8-yl)oxy]methyl}benzenesulfonamido)oxane-4-carbonyl]piperazin-1-yl}-5-oxopentyl)trimethylazanium chloride
Smiles: [Cl-].CC1C=C(C)N=C2C(=CC=CC=12)OCC1C(Cl)=CC=C(C=1Cl)S(=O)(=O)NC1(CCOCC1)C(=O)N1CCN(CC1)C(=O)C(N)CCC[N+](C)(C)C
InChiKey: ZNHJDJYKDVGQSH-UHFFFAOYSA-M
InChi: InChI=1S/C36H49Cl2N6O6S.ClH/c1-24-22-25(2)40-33-26(24)8-6-10-30(33)50-23-27-28(37)11-12-31(32(27)38)51(47,48)41-36(13-20-49-21-14-36)35(46)43-17-15-42(16-18-43)34(45)29(39)9-7-19-44(3,4)5;/h6,8,10-12,22,29,41H,7,9,13-21,23,39H2,1-5H3;1H/q+1;/p-1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. Fasitibant chloride inhibits the phosphorylation of FRSα, ERK1/2, STAT3 (BK induced; 1 μM; for 15 min), except AKT in HUVEC.
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.
Products are for research use only. Not for human use.
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