Product Data Sheet
Product Name:Rolapitant
me too是什么意思Cat. No.:GC15449
Chemical Properties
Cas No.552292-08-7摄影师培训学校
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
Canonical SMILES C[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
Formula C25H26F6N2O2M.Wt500.48 Solubility Soluble in DMSO Storage Store at -20°C
外贸业务员简历模板
General tips For obtaining a higher solubility , plea warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for veral months.subsidiary
游戏设计学校Shipping Condition Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request.
surveillanceStructure
Background Description: Kb: 0.17 nM
Product Data Sheet
六级阅读技巧Neurokinin NK1 receptors have been shown to play a role in a variety of behavioral respons in both animals and humans that has lead to the development of lective 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, lective 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 lectivity over the human NK2 and NK3 of >1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over mou, rat and rabbit. Rolapitant is a functionally competitive antagonist with a calculated Kb of 0.17 nM. [1].
尺子英文In vivo: Rolapitant reverd NK1 agonist-induced foot tapping in gerbils following both intravenous and oral administration up to 24 hours at a minimal effective do 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 do-dependent manner. No differences were obrved in side effect profile between rolapitant and placebo [2].
Reference:中考英语试题及答案
[1] Duffy RA, Morgan C, Naylor R, Higgins GA, Varty GB, Lachowicz JE, Parker EM. Rolapitant (SCH 619734): a potent, lective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100.
cect[2] Gan TJ, Gu J, Singla N, Chung F, Pearman MH, Berge SD, Habib AS, Candiotti KA, Mo Y, Huyck S, Creed MR, Cantillon M; Rolapitant Investigation Group. Rolapitant for the prevention of postoperative naua and vomiting: a prospective, double-blinded, placebo-controlled randomized trial. Anesth Analg. 2011 Apr;112(4):804-12.
