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Rolapitant

现货
Catalog No.
B5910
神经激肽NK1受体拮抗剂
组合的产品项目
规格价格库存 数量
25mg
¥ 5,520.00
Ship with 10-15 days
5mg
¥ 1,740.00
Ship with 10-15 days

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Background

Description:

Kb: 0.17 nM

Neurokinin NK1 receptors have been shown to play a role in a variety of behavioral responses in both animals and humans that has lead to the development of selective antagonists for this receptor. Principal of NK1 antagonists is their inhibitory effects against emesis induced by a variety of emetogenic stimuli. Rolapitant (SCH 619734) is a potent, selective and orally active neurokinin NK1 receptor antagonist.

In vitro: In vitro studies indicate that rolapitant has a high affinity for the human NK1 receptor of 0.66 nM and high selectivity over the human NK2 and NK3 of >1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over mouse, rat and rabbit. Rolapitant is a functionally competitive antagonist with a calculated Kb of 0.17 nM. [1].

In vivo: Rolapitant reversed NK1 agonist-induced foot tapping in gerbils following both intravenous and oral administration up to 24 hours at a minimal effective dose of 0.1 mg/kg. Rolapitant was efficacious at 0.1 and 1 mg/kg in both acute and delayed emesis models in ferrets, respectively, which is consistent with clinical data for other NK1 antagonists [1].

Clinical trial: Rolapitant is superior to placebo in reducing emetic episodes after surgery and reduces the incidence of vomiting in a dose-dependent manner. No differences were observed in side effect profile between rolapitant and placebo [2].

Reference:
[1] Duffy RA, Morgan C, Naylor R, Higgins GA, Varty GB, Lachowicz JE, Parker EM.  Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100.
[2] Gan TJ, Gu J, Singla N, Chung F, Pearman MH, Bergese SD, Habib AS, Candiotti KA, Mo Y, Huyck S, Creed MR, Cantillon M; Rolapitant Investigation Group.  Rolapitant for the prevention of postoperative nausea and vomiting: a prospective, double-blinded, placebo-controlled randomized trial. Anesth Analg. 2011 Apr;112(4):804-12.

Chemical Properties

StorageStore at -20°C
M.Wt500.48
Cas No.552292-08-7
FormulaC25H26F6N2O2
SolubilitySoluble in DMSO
Chemical Name(5S,8S)-8-(((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro[4.5]dec-1-en-2-ol
SDFDownload SDF
Canonical SMILESC[C@](OC[C@@]1(C2=CC=CC=C2)CC[C@@]3(CN1)CCC(O)=N3)([H])C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

质量控制和MSDS

批次:

化学结构

Rolapitant