GSK1292263

生物活性体外研究体内研究生物活性靶点体外研究体内研究 GSK1292263 试剂级价格

GSK1292263

CAS号:1032823-75-8
英文名:GSK1292263
中文名:GSK1292263
CBNumber:CB82522975
分子式:C23H28N4O4S
分子量:456.56
MOL File:1032823-75-8.mol

GSK1292263化学性质

沸点 :655.1±65.0 °C(Predicted)
密度 :1.23
储存条件 :Store at -20°C
溶解度 :≥21.1 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
形态 :solid
酸度系数(pKa) :4.75±0.32(Predicted)
颜色 :White to off-white

GSK1292263性质、用途与生产工艺

生物活性 GSK1292263是一种新型GPR119激动剂，用于治疗2型糖尿病。Phase 2。
体外研究 GSK-1292263 is selected from 1538 compounds by using Hypo1, the Fit-Value and Estimate of GSK-1292263 that is aligned in Hypo1 are 8.8 and 7.7 (nM), respectively.
体内研究 GSK-1292263 administrated at a single dose of 3-30 mg/kg in the absence of nutrients correlates with increased levels of circulating gastrointestinal peptides, including glucagon-like peptide 1 (GLP-1), gastric inhibitory polypeptide (GIP), peptide YY (PYY) and glucagon in male Sprague-Dawley rats, the increase is enhanced following administration of glucose in the oral glucose tolerance test (OGTT). GSK-129226 significant increases in the peak insulin response and insulin AUC(0-15 min) of 30-60% compared with values in the vehicle control cohort in the intravenous glucose tolerance test in rats, this insulin upregulation correlated with a significant increase in the glucose disposal rate. GSK-1292263 is associated with a statistically significant increase in insulin immunoreactivity in pancreatic sections in a 6-week study performed in Zucker diabetic fatty rats, compared with insulin immunoreactivity in samples obtained from rats receiving vehicle control. GSK-1292263 administrated at dose of 10 or 30 mg/kg or vehicle control at 2 hours prior to insulin infusion in hyperinsulinemic-euglycemic clamps stimulates glucagon secretion without increasing blood glucose levels Sprague-Dawley rats.
生物活性 GSK1292263是一种新型GPR119激动剂，用于治疗2型糖尿病。Phase 2。
靶点
Target Value
GPR119
()
体外研究
GSK-1292263通过使用Hypo1从1538种化合物中被选出，与Hypo1中一致的GSK-1292263的拟合值和估计值分别为8.8和7.7 (nM)。
体内研究在雄性Sprague-Dawley大鼠体内，GSK-1292263(3-30 mg/kg)以单剂量给药在营养素不存在时，与循环胃肠肽，包括胰高血糖素样多肽1(GLP-1)，肠抑胃肽(GIP)，多肽YY (PYY)和胰高血糖素的增加水平相关，在口服葡萄糖耐量测试(OGTT)中，葡萄糖给药会加强循环胃肠肽的增加。在大鼠静脉内葡萄糖耐量测试中，GSK-129226显著增加胰岛素反应的峰值，并且与载体对照组相比，增加30-60%的胰岛素AUC(0-15 min)，此处胰岛素的上调与葡萄糖清除率的显著增加相关。在Zucker糖尿病肥胖大鼠的6周研究中，与空白对照大鼠样本中胰岛素免疫反应性相比，GSK-1292263与胰腺切片中胰岛素免疫反应性在统计学上的显著增加相关。Sprague-Dawley大鼠体内，高胰岛素-正常血糖钳夹实验中，胰岛素注射2小时前，GSK-1292263以10 或30 mg/kg的剂量给药或与载体对照相比，刺激胰高血糖素分泌，而不增加血糖水平。