西他列汀磷酸盐
磷酸西他列汀(sitagliptin phosphate)
CAS: 654671-78-0;847445-79-8
化学式: C16H15F6N5O.H3PO4
| 中文名 | 磷酸西他列汀 |
| 英文名 | sitagliptin phosphate |
| 别名 | 磷酸西他列汀 西他列汀磷酸盐 无水磷酸西他列汀 磷酸西他列汀无水物 磷酸西他列汀(降糖药) 磷酸西他列汀原料药和中间体 磷酸西他列汀 磷酸西他列汀一水化物 4-氧代-4-(3-三氟甲基-5,6-二氢(1,2,4)三唑并[4,3-a]吡嗪-7(8H)-基)-1-(2,4,5-三氟苯基)丁-2-胺磷酸盐 7-[(3R)-3-氨基-1-氧代-4-(2,4,5-三氟苯基)丁基]-5,6,7,8-四氢-3-三氟甲基-1,2,4-三唑并[4,3-a]吡嗪磷酸盐 |
| 英文别名 | sitagpliptin sitagliptin phosphate Sitagliptin phosphate sitagliptin phosphate intermediates 3-Amino-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]-pyrazin-7(8H)-yl)-4-(2,4,5-t (3R)-3-aMino-1-[3-(trifluoroMethyl)-5H,6H,7H,8H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one 4-Oxo-4-(3-(trifluoromethyl)-5,6-dihydro(1,2,4)triazolo[4,3-a]pyrazin-7(8H)-yl)-1-(2,4,5-trifluorophenyl)butan-2-amine phosphate 7-[(3R)-3-Amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine phosphate 7-[(3R)-3-Amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine-phosphate 7-[(3R)-3-Amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-α]pyrazine-phosphate (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine phosphate Sitagliptin phosphate 4-Oxo-4-(3-(trifluoromethyl)-5,6-dihydro(1,2,4)triazolo[4,3-a]pyrazin-7(8H)-yl)-1-(2,4,5-trifluorophenyl)butan-2-amine phosphate |
| CAS | 654671-78-0 847445-79-8 |
| EINECS | 1806241-263-5 |
| 化学式 | C16H15F6N5O.H3PO4 |
| 分子量 | 505.31 |
| InChI | InChI=1/C16H15F6N5O.H3O4P/c17-10-6-12(19)11(18)4-8(10)3-9(23)5-14(28)26-1-2-27-13(7-26)24-25-15(27)16(20,21)22;1-5(2,3)4/h4,6,9H,1-3,5,7,23H2;(H3,1,2,3,4)/t9-;/m1./s1 |
| 熔点 | 202-204°C |
| 沸点 | 529.9°C at 760 mmHg |
| 闪点 | 274.3°C |
| 蒸汽压 | 2.59E-11mmHg at 25°C |
| 溶解度 | 甲醇 (轻微加热)，水 (微溶，超声处理) |
| 存储条件 | -20°C Freezer |
| 外观 | 固体 |
| 颜色 | White to Off-White |
| 物化性质 |
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| 体外研究 | Sitagliptin phosphate exhibits a potent inhibitory effect on DPP-4 with IC 50 of 19 nM from Caco-2 cell extracts.Sitagliptin reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation.A recent study demonstrates that sitagliptin exerts a novel, direct action in order to stimulate GLP-1 secretion by the intestinal L cell through a DPP-4-independent, protein kinase A- and MEK-ERK1/2-dependent pathway. It therefore reduces the effect of autoimmunity on graft survival. |
| 体内研究 | In vivo, the ED 50 value of sitagliptin phosphate for inhibition of plasma DPP-4 activity is calculated to be 2.3 mg/kg 7 hour postdose and 30 mg/kg 24 hour postdose in freely fed Han-Wistar rats.The streptozotocin-induced type 1 diabetes mouse model exhibits elevated DPP-4 levels in the plasma that can be substantially inhibited in mice on an Sitagliptin phosphate diet. This is achieved by a positive effect on the regulation of hyperglycemia, potentially through prolongation of islet graft survival.The plasma clearance and volume of distribution of Sitagliptin phosphate are higher in rats (40-48 mL/min/kg, 7-9 L/kg) than in dogs (9 mL/min/kg, 3 L/kg); and its half-life is shorter in rats,2 hours compared with 4 hours in dogs. |
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