產(chǎn)品屬性：
產(chǎn)品名稱 | rac-Aprepitant-d4 |
規(guī)格 | 500 μg、1 mg |
貨號 | EY-01Y17549 |
Cas No.: N/A
別名: N/A
化學(xué)名: N/A
分子式: C23H17D4F7N4O3
分子量: 538.5
溶解度: DMF: 25 mg/ml,DMSO: 16 mg/ml,Ethanol: 3 mg/ml
儲存條件: -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述：
rac-Aprepitant-d4 is intended for use as an internal standard for the quantification of aprepitant by GC- or LC-MS. Aprepitant an antiemetic compound and antagonist of the neurokinin-1 (NK1) receptor (Ki = 3 nM; IC50 = 0.09 nM for the human receptor).1,2 It is selective for NK1 over NK3 receptors (Ki = 454.1 nM for human NK3).1 In vivo, aprepitant (1 mg/kg) prevents plasma extravasation into the esophagus of guinea pigs induced by substance P .3 It also reduces NK1-agonist-induced foot tapping in gerbils. Formulations containing aprepitant have been used to prevent chemotherapy-induced nausea and vomiting.1.Bissantz, C., Bohnert, C., Hoffmann, T., et al.Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK1/NK3 antagonistsJ. Med. Chem.55(11)5061-5076(2012)
2.Finke, P.E., Meurer, L.C., Levorse, D.A., et al.Cyclopentane-based human NK1 antagonists. Part 1: Discovery and initial SARBioorg. Med. Chem. Lett.16(17)4497-4503(2006)
3.Meurer, L.C., Finke, P.E., Owens, K.A., et al.Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivativesBioorg. Med. Chem. Lett.16(17)4504-4511(2006)
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