Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Gosogliptin is a potent and selective dipeptidyl peptidase-IV (DPP-IV) inhibitor.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | Gosogliptin is a potent and selective dipeptidyl peptidase-IV (DPP-IV) inhibitor. |
体外活性 | Gosogliptin demonstrates greater than 200-fold selectivity over other members of the DPP family (DPP-2, DPP-3, DPP-8, and DPP-9) and the related serine proteases, fibroblast activation protein, aminopeptidase P, and propyl oligopeptidase, enzymes that possess similar catalytic activities.?Gosogliptin demonstrates rapid and reversible inhibition of plasma DPP-4 activity when administered orally to rats, dogs, and monkeys.?In various nonclinical models, Gosogliptin stimulates insulin secretion and improves glucose tolerance.Gosogliptin ?is a potent, orally active, selective, and competitive inhibitor of DPP-IV, the enzyme mainly responsible for the degradation of the incretin peptides GLP-1 and glucose-dependent insulinotropic polypeptide. |
体内活性 | The objectives of the present study are to characterize the metabolism, pharmacokinetics, and excretion of Gosogliptin in Sprague-Dawley ?rats, beagle dogs, and humans.?A single dose of ?Gosogliptin is administered orally to intact SD rats (5 mg/kg), beagle dogs (5 mg/kg), and humans (20 mg).?After a single oral dose of ?Gosogliptin to SD rats, an overall mean of 97.1% of the administered radioactivity is recovered in the urine, feces, and cage wash over a period of 168 h postdose.?The mean cumulative dose recovered in feces is 66.0%.?The mean cumulative excretion in the urine is 30.8%.?Approximately 95% of the excreted radioactivity recovery occurred in the first 48 h. Mean total recoveries of dosed radioactivity from bile duct-cannulated rats are 29.5% in urine and 62.0% in bile.?No gender-related differences are observed in the excretion pattern of radioactivity. |
别名 | PF-00734200, PF-734200 |
分子量 | 366.41 |
分子式 | C17H24F2N6O |
CAS No. | 869490-23-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Gosogliptin 869490-23-3 Others PF00734200 PF-00734200 PF 00734200 PF-734200 PF 734200 PF734200 Inhibitor inhibitor inhibit