中文名福沙吡坦二甲葡胺
英文名Fosaprepitant Dimeglumine
别名福沙匹坦二葡jiaan
福沙吡坦二甲葡胺
福沙匹坦二甲葡胺
福沙匹坦(API)
福沙匹坦二甲葡胺对照品
福沙吡坦二甲葡胺及全套杂质
福沙吡坦二甲葡胺(MK-0517)
1-脱氧-1-(甲基氨基)-D-葡萄糖醇 [3-[[(2R,3S)-2-[(1R)-1-[3,5-双(三氟甲基)苯基]乙氧基]-3-(4-氟苯基)-4-吗啉基]甲基]-2,5-二氢-5-氧代-1H-1,2,4-三唑-1-基]膦酸盐
英文别名MK-0517
Ivemend
Unii-D35fm8T64x
UNII-D35FM8T64X
Fosaprepitant Dimeglumine
Fosaprepitant diMegluMine salt
Fosaprepitant dimeglumine [USAN]
1-DEOXY-1-(METHYLAMINO)-D-GLUCITOL [[(2R,3S]-2-[(1R)-1-[3,5-BIS (TRIFLUOROMETHYL)PHENYL] PHENYL]ETHOXY]-(4-FLUOROPHENYL)
3-[2(R)-[1(R)-[3,5-Bis(trifluoroMethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)Morpholin-4-ylMethyl]-5-oxo-4,5-dihydro-1H-1,2,4-triazole-1-phosphinic acid bis(N-Methyl-D-glucaMine) salt
[3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoroMethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-Morpholinyl]Methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]phosphonate 1-Deoxy-1-(MethylaMino)-D-glucitol
1-Deoxy-1-(MethylaMino)-D-glucitol [3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoroMethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-Morpholinyl]Methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]phosphonate
1-Deoxy-1-(Methylamino)-D-Glucitol [3-[[(2R,3S)-2-[(1R)-1-[3,5-Bis(Trifluoromethyl)Phenyl]Ethoxy]-3-(4-Fluorophenyl)-4-Morpholinyl]Methyl]-2,5-Dihydro-5-Oxo-1H-1,2,4-Triazol-1-Yl]Phosphonate
CAS265121-04-8
EINECS682-419-4化学式C60H78F14N10O20P2
分子量1587.2414868InChIInChI=1/C23H22F7N4O6P.2C7H17NO5/c1-12(14-8-15(22(25,26)27)10-16(9-14)23(28,29)30)40-20-19(13-2-4-17(24)5-3-13)33(6-7-39-20)11-18-31-21(35)34(32-18)41(36,37)38;2*1-8-2-4(10)6(12)7(13)5(11)3-9/h2-5,8-10,12,19-20H,6-7,11H2,1H3,(H,31,32,35)(H2,36,37,38);2*4-13H,2-3H2,1H3/t12-,19+,20-;2*4-,5+,6+,7+/m100/s1酸度系数Fosaprepitant dimeglumine has four functional groups which have pKa values of 3.05 ± 0.03, 4.92 ± 0.存储条件Sealed in dry,Store in freezer, under -20°C体外研究Fosaprepitant (MK-0517, L-758,298)是一种aprepitant的磷酰基前药。Aprepitant是一种选择性P物质(NK-1 受体)拮抗剂，被批准用作与皮质类固醇和 5-HT 3受体拮抗剂的联合疗法，以预防急性和延迟化疗诱导的恶心和呕吐。体内研究Fosaprepitant静脉内给药30分钟内通过常见磷酸酶的作用转化为aprepitant。Fosaprepitant在高达150 mg (1 mg/ml)剂量下耐受性良好，Fosaprepitant 115 mg在其AUC中生物等效于aprepitant 125 mg。Fosaprepitant 115 mg已经被提交到FDA，作为aprepitant口服给药3天疗程里第1天代替给药，aprepitant在第2和第3天口服给药。