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Rolapitant hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Rolapitant hydrochloride图片
CAS NO:858102-79-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
罗拉匹坦盐酸盐
SCH619734 hydrochloride
产品介绍
Rolapitant (SCH619734) hydrochloride 是一种长效且具有选择性和口服活性的神经激肽 1 (NK1) 受体拮抗剂,Ki值为 0.66 nM。Rolapitant hydrochloride 不与 CYP3A4 产生互作。Rolapitant hydrochloride 在雪貂呕吐模型中显示出强效的止吐活性。
生物活性

Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally activeneurokinin 1 (NK1) receptorantagonist with aKiof 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model[1][2].

IC50& Target[1]

human NK1

0.66 (Ki)

gerbil NK1

0.13 (Ki)

guinea pig NK1

0.72 (Ki)

monkey NK1

2.5 (Ki)

rabbit NK1

31.7 (Ki)

rat NK1

78.6 (Ki)

mouse NK1

60.4 (Ki)

体外研究
(In Vitro)

Rolapitant has high selectivity over the human NK2 and NK3 subtypes of more than 1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit[1].
Rolapitant (1-1000 nM) inhibits the GR-73632 (an NK1 receptor agonist)-induced calcium efflux with a concentration-dependent and competitive manner in CHO cells expressing the human NK1 receptor[1].

体内研究
(In Vivo)

Rolapitant (0.03-1 mg/kg for PO, 0.3-1 mg/kg for IV; single dosage) attenuates the GR-73632-induced foot-tapping response in Mongolian Gerbils[1].
Rolapitant (0.03-1 mg/kg; PO; single dosage; observed for 72 h) blocks acute emesis induced by both apomorphine and cisplatin in ferrets[1].

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)[1]
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 ID90of 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)[1]
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.
Clinical Trial
分子量

536.94

Formula

C25H27ClF6N2O2

CAS 号

858102-79-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.