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

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.

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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].

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.
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
References
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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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