Fabesetron (Synonyms: FK1052 free base)

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Data Sheet SDS COA Handling Instructions

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Fabesetron (FK1052) is an orally active 5-HT₃ receptor antagonist with 5-HT₄ receptor antagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced by cancer chemotherapy.

For research use only. We do not sell to patients.

Fabesetron Chemical Structure

CAS No. : 129300-27-2

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Description

IC₅₀ & Target^[1]

5-HT₃ Receptor

5-HT₄ Receptor

In Vivo

Fabesetron (FK1052) (0.1 mg/kg p.o.) inhibits completely the increases in the colonic transit^[1].
FK1052 (100 µg/kg) completely prevents emesis induced by cisplatin (18 mg/kg, i.p.) in Suncus murinus^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley rats weighing 220 to 330 g and male ddy mice weighing 25 to 35 g were used^[1].
Dosage:	0.1 mg/kg.
Administration:	P.O.
Result:	Significantly caused delay and its degree of inhibition was 33.8 ± 4.8% by 0.1 mg/kg p.o..

Animal Model:	Suncus murinus of either sex (>10-week-old; 30-70 g body weight)^[2].
Dosage:	1, 10, and 100 µg/kg.
Administration:	Orally administered 30 min before the injection of cisplatin.
Result:	Inhibited cisplatininduced emesis in a dose-dependent manner, and no emesis was observed in three animals given the compound at 100 µg/kg.

Molecular Weight

293.36

Formula

C₁₈H₁₉N₃O

CAS No.

129300-27-2

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1N2C3=C(C=CC=C3)C(C)=C2CC[C@@H]1CC4=C(NC=N4)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Purity & Documentation

Purity: 95.72%

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Data Sheet (271 KB) SDS (251 KB)

COA (247 KB) HNMR (99 KB) RP-HPLC (95 KB) MS (105 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

Fabesetron Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fabesetron129300-27-2FK1052FK 1052FK-10525-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorcancerchemotherapyemesisInhibitorinhibitorinhibit

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