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/ Sitagliptin phosphate monohydrate

西他列汀磷酸盐一水合物 /Sitagliptin phosphate monohydrate {[allProObj[0].p_purity_real_show]}

货号：A323507 同义名： 磷酸西他列汀一水合物 / MK-0431;MK-0431 phosphate monohydrate

Sitagliptin Phosphate Monohydrate is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts.

Sitagliptin phosphate monohydrate 化学结构 CAS号：654671-77-9
Sitagliptin phosphate monohydrate 化学结构
CAS号：654671-77-9
Sitagliptin phosphate monohydrate 3D分子结构
CAS号：654671-77-9
Sitagliptin phosphate monohydrate 化学结构 CAS号：654671-77-9
Sitagliptin phosphate monohydrate 3D分子结构 CAS号：654671-77-9
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Sitagliptin phosphate monohydrate 纯度/质量文件 产品仅供科研

货号：A323507 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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Sitagliptin phosphate monohydrate 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].

Sitagliptin phosphate monohydrate 动物研究

Dose Rat: 20 mg/kg[3] (p.o.)
Administration p.o.

Sitagliptin phosphate monohydrate 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 - -

Sitagliptin phosphate monohydrate 参考文献

[1]Sitagliptin

[2]Ertugliflozin and Sitagliptin

[3]Sitagliptin

Sitagliptin phosphate monohydrate 实验方案

计算器
存储液制备 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

Sitagliptin phosphate monohydrate 技术信息

CAS号654671-77-9
分子式C16H20F6N5O6P
分子量 523.324
别名 磷酸西他列汀一水合物 ;MK-0431;MK-0431 phosphate monohydrate
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
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

Tags: Sitagliptin phosphate | 654671-77-9 | MK-0431 phosphate | DPP4 Inhibitor | Metabolic Enzyme/Protease | Autophagy | Dipeptidyl Peptidase | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Sitagliptin phosphate monohydrate 纯度/质量文件 | Sitagliptin phosphate monohydrate 生物活性 | Sitagliptin phosphate monohydrate 动物研究 | Sitagliptin phosphate monohydrate 临床数据 | Sitagliptin phosphate monohydrate 参考文献 | Sitagliptin phosphate monohydrate 实验方案 | Sitagliptin phosphate monohydrate 技术信息

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