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.
For research use only. We do not sell to patients.
- CAS No.: 129300-27-2
- Formula: C18H19N3O
- Molecular Weight:293.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
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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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CAS No. 129300-27-2
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Appearance Solid
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Molecular Weight 293.36
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (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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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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fabesetron Related Classifications
HY-105201 Related Classifications
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