货号	规格	价格	上海	北京	珠海	重庆	武汉
S85739-1mg买3赠1	99.80%	￥260.00 S85739-1mg ￥260.00 现货（买3赠1）	8 8	-	-	-	-
S85739-5mg买3赠1	99.80%	￥570.00 S85739-5mg ￥570.00 现货（买3赠1）	6 6	-	-	-	-
S85739-10mg买3赠1	99.80%	￥880.00 S85739-10mg ￥880.00 现货（买3赠1）	6 6	-	-	-	-
S85739-25mg买3赠1	99.80%	￥1800.00 S85739-25mg ￥1800.00 现货（买3赠1）	7 7	-	-	-	-
S85739-50mg买3赠1	99.80%	￥2700.00 S85739-50mg ￥2700.00 现货（买3赠1）	5 5	-	-	-	-
S85739-100mg买3赠1	99.80%	￥3750.00 S85739-100mg ￥3750.00 现货（买3赠1）	4 4	-	-	-	-

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产品描述：

Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model

靶点：

human NK1:0.66 nM (Ki);gerbil NK1:0.13 nM (Ki);guinea pig NK1:0.72 nM (Ki);monkey NK1:2.5 nM (Ki);rabbit NK1:31.7 nM (Ki);rat NK1:78.6 nM (Ki);mouse NK1:60.4 nM (Ki);Neurokininreceptor

体外研究：

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. 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

体内研究：

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. Rolapitant (0.03-1 mg/kg; PO; single dosage; observed for 72 h) blocks acute emesis induced by both apomorphine and cisplatin in ferrets. 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.

参考文献：

1. Duffy RA, et al. Rolapitant (SCH 619734): a potent, selective and orally active neurokininNK1 receptor antagonist with centrally-mediated antiemetic effects inferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100. 2. Rapoport B, et al. Study of rolapitant, a novel, long-acting, NK-1 receptor antagonist, for the prevention of chemotherapy-induced nausea and vomiting (CINV) due to highly emetogenic chemotherapy (HEC). Support Care Cancer. 2015 Nov;23(11):3281-8.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.998 ml	9.99 ml	19.981 ml
5 mM	0.4 ml	1.998 ml	3.996 ml
10 mM	0.2 ml	0.999 ml	1.998 ml
50 mM	0.04 ml	0.2 ml	0.4 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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