Name | Fosaprepitant |
Synonyms | L 758298 Fosaprepitant MK-0517 (Fosaprepitant) Fosaprepitant(See also F727305) [3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-2H-1,2,4-triazol-1-yl]phosphonic acid [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]phosphonic acid (3-{[(2R,3S)-2-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}-3-(4-fluorophenyl)morpholin-4-yl]methyl}-5-oxo-2,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid P-[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]phosphonic Acid |
CAS | 172673-20-0 |
InChI | InChI=1/C23H22F7N4O6P/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/h2-5,8-10,12,19-20H,6-7,11H2,1H3,(H,31,32,35)(H2,36,37,38)/t12-,19+,20-/m1/s1 |
Molecular Formula | C23H22F7N4O6P |
Molar Mass | 614.41 |
Density | 1.65 |
Melting Point | >74°C (dec.) |
Boling Point | 588.9°C at 760 mmHg |
Flash Point | 310°C |
Solubility | DMSO, Methanol |
Vapor Presure | 1.03E-14mmHg at 25°C |
Appearance | Solid |
Color | White |
pKa | 2.45±0.20(Predicted) |
Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
Refractive Index | 1.589 |
biological activity | Fosaprepitant (L-758298) is a prodrug for Aprepitant (HY-10052). Fosaprepitant is a neurokinin-1 receptor (neurokinin-1 receptor) antagonist developed to prevent chemotherapy-induced nausea and vomiting (CINV). |
target | Neurokinin-1 receptor |
Animal Model: | Sprague-Dawley rats |
Dosage: | 30 mg/kg |
Administration: | Intraperitoneal injection, daily, for 7 days |
Result: | Increased the antinociceptive effect of morphine compared to control group. |