1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Fabesetron

Fabesetron (Synonyms: FK1052 free base)

Cat. No.: HY-105201 Purity: 95.72%
Handling Instructions

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

Fabesetron Chemical Structure

CAS No. : 129300-27-2

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Description

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[1][2].

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].

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

SMILES

O=C1N2C3=C(C=CC=C3)C(C)=C2CC[[email protected]@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
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Keywords:

FabesetronFK1052FK 1052FK-10525-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorcancerchemotherapyemesisInhibitorinhibitorinhibit

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Fabesetron
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HY-105201
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