产品说明书
Sitagliptin phosphate monohydrate
 |
同义名 : | 磷酸西他列汀一水合物 ;MK-0431;MK-0431 phosphate monohydrate |
| CAS号 : | 654671-77-9 | |
| 货号 : | A323507 | |
| 分子式 : | C16H20F6N5O6P | |
| 纯度 : | 99% | |
| 分子量 : | 523.324 | |
| MDL号 : | MFCD19684081 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
H2O: 30 mg/mL(57.33 mM) |
|
| 动物实验配方： |
PO 0.5% CMC-Na 30 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Sitagliptin, the first selective DPP-4 (dipeptidyl peptidase-4) inhibitor approved by the US FDA in 2006 for treatment of type 2 diabetes mellitus, has an IC50 value of 18 nM for DPP-4, which is much more selective than DPP-8 and DPP-9. DPP-4 is a serine peptidase located on the cell surface and is widely distributed in plasma, gastrointestinal tract, kidney, lymph nodes and connective tissue. GLP-1 and GIP can be rapidly inactivated by DPP-4 after secretion in the gastrointestinal tract. By inhibiting DPP-4, sitagliptin increases GLP-1 and GIP levels, while GLP-1 and GIP are glucose-dependent. In activation assays in murine T- and B-cells, sitagliptin did not inhibit T cell proliferation and alter LPS induced proliferation of B cells over a range of 12 nM to 50 nM[3]. In vivo, sitagliptin inhibited plasma DPP4 activity, increased plasma GLP-1 and reduced blood glucose excursion in a dose-dependent manner (plasma efficacious drug concentrations were 200 - 700 nM) with optimal dose of 1 mg/kg (46% inhibition), 3 mg/kg, 3 mg/kg in lean mice, DIO mice and db/db mouse respectively[3]. The oral bioavailability of sitagliptin is 60-90% in rats and dogs[4]. Other research has found that in streptozotocin induced diabetic male wistar rats (intravenous injection of 65 mg/kg 15 min after an intraperitoneal injection of 230 mg/kg nicotinamide), treatment with sitagliptin could significantly decrease the attenuates bone loss and improves mechanical bone strength as well as did not have any effect on glucose levels[5]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00541229 | Type 2 Diabetes | Phase 1 | Completed | - | - |
| NCT00961363 | Impaired Glucose Tolerance | Phase 2 | Unknown | - | Taiwan ... 展开 >> National Taiwan University Hospital Recruiting Taipei, Taiwan, 100 Contact: Lee-Ming Chuang, MD, PhD 886-2-23123456 ext 65038 leeming@ntu.edu.tw Principal Investigator: Lee-Ming Chuang, MD, PhD Sub-Investigator: Hung-Yuan Li, MD Sub-Investigator: Hung-Ju Lin, MD Sub-Investigator: Chia-Hsiung Chang, MD, PhD Sub-Investigator: Shyang-Rong Shih, MD Sub-Investigator: Tien-Jyun Chang, MD, PhD Sub-Investigator: Jaw-Shiun Tsai, MD 收起 << |
| NCT00541229 | - | Completed | - | - | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.91mL 0.38mL 0.19mL |
9.55mL 1.91mL 0.96mL |
19.11mL 3.82mL 1.91mL |
| 参考文献 |
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