Description
(±)-Fabesetron hydrochloride ((±)-FK1052) is the racemate of Fabesetron hydrochloride, which is a potent 5-HT3 and 5-HT4 receptor dual antagonist.
Product information
CAS Number: 129299-81-6
Molecular Weight: 329.82
Formula: C18H20ClN3O
Chemical Name: 10-methyl-7-[(4-methyl-1H-imidazol-5-yl)methyl]-6H,7H,8H,9H-pyrido[1,2-a]indol-6-one hydrochloride
Smiles: Cl.CC1N=CNC=1CC1CCC2=C(C)C3C=CC=CC=3N2C1=O
InChiKey: POKFYJWUPWZYQV-UHFFFAOYSA-N
InChi: InChI=1S/C18H19N3O.ClH/c1-11-14-5-3-4-6-17(14)21-16(11)8-7-13(18(21)22)9-15-12(2)19-10-20-15;/h3-6,10,13H,7-9H2,1-2H3,(H,19,20);1H
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 Vivo:
In conscious rats, both 5-HT and 5-methoxytryptamine significantly increase fecal pellet output and accelerate colonic transit. In contrast, the effect of 2-methyl-5-HT is slight. Although Ondansetron and Granisetron slightly reduce 5-HT (1 mg/kg s.c.) stimulated colonic transit, (±)-Fabesetron, at 0.1 mg/kg p.o., inhibits completely the increases in the colonic transit. Furthermore, (±)-Fabesetron, Ondansetron and Granisetron significantly depress the increase in fecal pellet output caused by wrap-restraint stress, with ED50 values of 0.21, 3.0 and 1.1 mg/kg p.o., respectively. Intraperitoneal administration of 5-HT and 5-methoxytryptamine, but not 2-methyl-5-HT, produces a dose-related increase in the incidence of diarrhea in fasted mice. 5-HT (0.32 mg/kg i.p.)-induced diarrhea is also inhibited by (±)-Fabesetron, Ondansetron and Granisetron, with ED50 values of 0.09, 2.3 and 0.88 mg/kg p.o., respectively. (±)-Fabesetron (1 mg/kg i.v. ×4) apparently reduces delayed emesis caused by Methotrexate (MTX) and increases, but not significantly, the time for onset of emesis. Furthermore, increasing the dose to 3.2 mg/kg of (±)-Fabesetron also significantly inhibits the number of the emetic episodes induced by MTX, of which the action is more effective than the treatment with (±)-Fabesetron at 1 mg/kg.
Products are for research use only. Not for human use.
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