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(±)-Fabesetron hydrochloride

Catalog No. T11293 CAS 129299-81-6

Synonyms: FK1052 hydrochloride

FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.

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(±)-Fabesetron hydrochloride Chemical Structure

(±)-Fabesetron hydrochloride, CAS 129299-81-6

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,970.00
50 mg	8-10 weeks	$ 2,580.00
100 mg	8-10 weeks	$ 3,400.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

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Description

FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.

In vivo

FK1052 (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 FK1052 also significantly inhibits the number of the emetic episodes induced by MTX, of which the action is more effective than the treatment with FK1052 at 1 mg/kg.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, FK1052, at 0.1 mg/kg p.o., inhibits completely the increases in the colonic transit.?Furthermore, FK1052, 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 FK1052, Ondansetron and Granisetron, with ED50 values of 0.09, 2.3 and 0.88 mg/kg p.o., respectively.

Synonyms	FK1052 hydrochloride
Molecular Weight	329.82
Formula	C18H20ClN3O
CAS No.	129299-81-6

Storage

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

References and Literature

1. Kadowaki M, 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. Yamakuni H, et al. Probable involvement of the 5-hydroxytryptamine(4) receptor in methotrexate-induced delayed emesis in dogs. J Pharmacol Exp Ther. 2000 Mar;292(3):1002-7.

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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 hydrochloride 129299-81-6 GPCR/G Protein Neuroscience 5-HT Receptor Fabesetron Hydrochloride (±) Fabesetron hydrochloride FK-1052 Hydrochloride FK1052 Hydrochloride FK1052 hydrochloride (±)Fabesetron hydrochloride FK 1052 Hydrochloride inhibitor inhibit

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