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Fabesetron (Synonyms: FK1052 free base)
Fabesetron (FK1052) 是具有口服活性的 5-HT3 和 5-HT4 受体的拮抗剂。Fabesetron (FK1052) 可用于癌症化疗引起的急性和迟发性呕吐的研究。
Fabesetron Chemical Structure
CAS No. : 129300-27-2
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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| 生物活性 |
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].
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| IC50 & Target[1] |
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5-HT3 Receptor
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5-HT4 Receptor
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体内研究
(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].
Shanghai Jinpan Biotech Co Ltd 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. |
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| 中文名称 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
| Powder |
-20°C |
3 years |
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4°C |
2 years |
| In solvent |
-80°C |
6 months |
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-20°C |
1 month |
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| 参考文献 |
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[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.
[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.
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