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Fabesetron

Catalog No. T38692 CAS 129300-27-2

Synonyms: FK1052 free base

Fabesetron (FK1052) is an orally active compound that acts as a dual antagonist, targeting both the 5-HT3 and 5-HT4 receptors. It exhibits efficacy in studying emesis induced by cancer chemotherapy, showing potential for managing both acute and delayed symptoms.

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Fabesetron, CAS 129300-27-2

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Description

In vivo

Fabesetron (FK1052) at a dose of 0.1 mg/kg when administered orally, effectively inhibits the increase in colonic transit in male Sprague-Dawley rats (220 to 330 g) and also completely prevents cisplatin (18 mg/kg, i.p.)-induced emesis in Suncus murinus (either sex, >10-week-old, 30-70 g). The study utilized male Sprague-Dawley rats and ddy mice for evaluating its effect on colonic transit, reporting a significant delay and inhibition degree of 33.8 ± 4.8% following a 0.1 mg/kg oral dose. In a dose-dependent manner, FK1052, administered orally 30 minutes before cisplatin, showed inhibited emesis in Suncus murinus, with no emesis observed at 100 μg/kg, indicating its potential for managing chemotherapy-induced side effects.

Synonyms	FK1052 free base
Molecular Weight	293.37
Formula	C18H19N3O
CAS No.	129300-27-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. M Kadowaki, et al. Effect of FK1052, a potent 5-hydroxytryptamine3 and 5-hydroxytryptamine4 receptor dual antagonist, on colonic function in vivo. J Pharmacol Exp Ther. 1993 Jul;266(1):74-80. 2. Hiroe Nakayama, et al. Antiemetic activity of FK1052, a 5-HT3- and 5-HT4-receptor antagonist, in Suncus murinus and ferrets. J Pharmacol Sci. 2005 Aug;98(4):396-403.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Fabesetron 129300-27-2 FK1052 free base FK-1052 FK1052 FK 1052 inhibitor inhibit

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