产品
编 号：F518045
分子式：C25H29ClF6N2O3
分子量：554.95
分子式：C25H29ClF6N2O3
分子量：554.95
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
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询价
100mg
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结构图
CAS No: 914462-92-3
产品详情
生物活性：
Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model.
体内研究：
Rolapitant hydrochloride hydrate (0.03-1 mg/kg for PO, 0.3-1 mg/kg for IV; single dosage) 减弱蒙古沙鼠中 GR-73632 (HY-P1192) 诱导的足部敲击反应。Rolapitant hydrochloride hydrate (0.03-1 mg/kg; PO; single dosage; observed for 72 h) 阻断雪貂中由阿扑吗啡和 cisplatin (HY-17394) 引起的急性呕吐。Animal Model:Female Mongolian Gerbils (30-60 g; anesthetized by inhalation of an oxygen:isofluorane mixture after 4 h PO or immediately after IV, then injected with 5 μl of 3 pmol solution of GR-73632 via ICV)
Dosage:0.03, 0.1, 0.3 and 1 mg/kg for PO, 0.3 and 1 mg/kg for IV
Administration:PO or IV, single dosage
Result:Attenuated dose-dependently the GR-73632-induced foot-tapping response when administered PO 4 h before testing, with an ID90 of 0.3 mg/kg, and the inhibition in foot tapping for at least 24 h.Blocked dose-dependently the foot tapping induced by GR-73632 when administered IV, with complete blockade observed at 1 mg/kg.
Animal Model:Ferrets (treated with subcutaneous administration of 0.125 mg/kg apomorphine or intraperitoneal administration of 10 mg/kg cisplatin)
Dosage:0.03, 0.1, 0.3 and 1 mg/kg
Administration:PO; single dosage; observed for 72 h
Result:Blocked dose-dependently acute emesis induced by both apomorphine and cisplatin in ferrets.Produced a robust decrease in retches and vomits in ferrets that was maintained throughout the 72 h observation period.
体外研究：
Rolapitant hydrochloride hydrate 对人类 NK2 和 NK3 亚型的选择性超过 1000 倍，并且对人类、豚鼠、沙鼠和猴子 NK1 受体的亲和力优于大鼠、小鼠和兔.Rolapitant hydrochloride hydrate (1-1000 nM) 在表达人 NK1 受体的 CHO 细胞中以浓度依赖性和竞争性方式抑制 GR-73632 (一种 NK1 受体激动剂) 诱导的钙流出。
Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model.
体内研究：
Rolapitant hydrochloride hydrate (0.03-1 mg/kg for PO, 0.3-1 mg/kg for IV; single dosage) 减弱蒙古沙鼠中 GR-73632 (HY-P1192) 诱导的足部敲击反应。Rolapitant hydrochloride hydrate (0.03-1 mg/kg; PO; single dosage; observed for 72 h) 阻断雪貂中由阿扑吗啡和 cisplatin (HY-17394) 引起的急性呕吐。Animal Model:Female Mongolian Gerbils (30-60 g; anesthetized by inhalation of an oxygen:isofluorane mixture after 4 h PO or immediately after IV, then injected with 5 μl of 3 pmol solution of GR-73632 via ICV)
Dosage:0.03, 0.1, 0.3 and 1 mg/kg for PO, 0.3 and 1 mg/kg for IV
Administration:PO or IV, single dosage
Result:Attenuated dose-dependently the GR-73632-induced foot-tapping response when administered PO 4 h before testing, with an ID90 of 0.3 mg/kg, and the inhibition in foot tapping for at least 24 h.Blocked dose-dependently the foot tapping induced by GR-73632 when administered IV, with complete blockade observed at 1 mg/kg.
Animal Model:Ferrets (treated with subcutaneous administration of 0.125 mg/kg apomorphine or intraperitoneal administration of 10 mg/kg cisplatin)
Dosage:0.03, 0.1, 0.3 and 1 mg/kg
Administration:PO; single dosage; observed for 72 h
Result:Blocked dose-dependently acute emesis induced by both apomorphine and cisplatin in ferrets.Produced a robust decrease in retches and vomits in ferrets that was maintained throughout the 72 h observation period.
体外研究：
Rolapitant hydrochloride hydrate 对人类 NK2 和 NK3 亚型的选择性超过 1000 倍，并且对人类、豚鼠、沙鼠和猴子 NK1 受体的亲和力优于大鼠、小鼠和兔.Rolapitant hydrochloride hydrate (1-1000 nM) 在表达人 NK1 受体的 CHO 细胞中以浓度依赖性和竞争性方式抑制 GR-73632 (一种 NK1 受体激动剂) 诱导的钙流出。
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