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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- No. CAS: 129300-27-2
- Fòrmula: C18H19N3O
- Peso molecular:293.36
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Ver todos los productos específicos de isoformas 5-HT Receptor
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Actividad biológica
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5-HT3 Receptor |
5-HT4 Receptor |
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.
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Animal Model:Male Sprague-Dawley rats weighing 220 to 330 g and male ddy mice weighing 25 to 35 g were used[1].
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Dosage:0.1 mg/kg.
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Administration:P.O.
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Result:Significantly caused delay and its degree of inhibition was 33.8 ± 4.8% by 0.1 mg/kg p.o..
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Animal Model:Suncus murinus of either sex (>10-week-old; 30-70 g body weight)[2].
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Dosage:1, 10, and 100 µg/kg.
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Administration:Orally administered 30 min before the injection of cisplatin.
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Result:Inhibited cisplatininduced emesis in a dose-dependent manner, and no emesis was observed in three animals given the compound at 100 µg/kg.
Chemical Information
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No. CAS 129300-27-2
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Appearance Solid
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Peso molecular 293.36
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Fòrmula C18H19N3O
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Color Off-white to light yellow
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SMILES
O=C1N2C3=C(C=CC=C3)C(C)=C2CC[C@@H]1CC4=C(NC=N4)C
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Synonyms
FK1052 free base
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Pureza y Documentación
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Ficha de datos (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fabesetron Related Classifications
HY-105201 Related Classifications
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