GSK1292263

GSK1292263

中文名称GSK1292263
中文同义词5-[[[1-(3-异丙基-1,2,4-二唑-5-基)-4-哌啶基]甲基]氧基]-2-[4-(甲磺酰基)苯基]吡啶;5-[[[1-(3-异丙基-1,2,4-恶二唑-5-基)-4-哌啶基]甲基]氧基]-2-[4-(甲磺酰基)苯基]吡啶;5-[[[1-(3-异丙基-1,2,4-噁二唑-5-基)-4-哌啶基]甲基]氧基]-2-[4-(甲磺酰基)苯基]吡啶;3-异丙基-5-(4-(((6-(4-(甲基磺酰)苯基)吡啶-3-基)氧基)甲基)哌啶-1-基)-1,2,4-恶二唑;化合物GSK1292263
英文名称GSK1292263
英文同义词3-Isopropyl-5-(4-(((6-(4-(methylsulfonyl)phenyl)pyridin-3-yl)oxy)methyl)piperidin-1-yl)-1,2,4-;5-[[[1-[3-(1-Methylethyl)-1,2,4-oxadiazol-5-yl]-4-piperidinyl]methyl]oxy]-2-[4-(methylsulfonyl)phenyl]pyridine;3-isopropyl-5-(4-(((6-(4-(Methylsulfonyl)phenyl)pyridin-3-yl)oxy)Methyl)piperidin-1-yl)-1,2,4-oxadiazole;3-Isopropyl-5-(4-(((6-(4-(methylsulfonyl)phenyl)pyridin-3-yl)oxy)methyl)piperidin-1-yl)-1,2,4-oxa;GSK1292263;5-((1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl)methoxy)-2-(4-(methylsulfonyl)phenyl)pyridine;5-[[[1-[3-(1-Methylethyl)-1,2,4-oxadiazol-5-yl]-4-piperidinyl]methyl]oxy]-2-[4-(methylsulfonyl)phenyl]pyridine gsk 1292263;CS-417
CAS号1032823-75-8
分子式C23H28N4O4S
分子量456.56
EINECS号
相关类别小分子抑制剂,天然产物;内分泌与激素;小分子抑制剂;Inhibitors
Mol文件1032823-75-8.mol
结构式GSK1292263 结构式

GSK1292263 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DMSO 中≥21.1 mg/mL;不溶于水;不溶于乙醇
形态固体
酸度系数(pKa)4.75±0.32(Predicted)

GSK1292263 用途与合成方法

GSK1292263是一种新型GPR119激动剂,用于治疗2型糖尿病。Phase 2。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.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.GSK1292263是一种新型GPR119激动剂,用于治疗2型糖尿病。Phase 2。
TargetValue
GPR119
()

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)。

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。

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-12066GSK1292263
GSK1292263
1032823-75-85mg800元
2024/01/25HY-12066GSK1292263
GSK1292263
1032823-75-810mM * 1mLin DMSO804元

GSK1292263 上下游产品信息

"GSK1292263"相关产品信息
GSK2126458 GSK2606414 AT7519 司美替尼 SGX-523 盐酸苯乙福明 2-氨基-8-[反式-4-(2-羟基乙氧基)环己基]-6-(6-甲氧基-3-吡啶基)-4-甲基吡啶并[2,3-D]嘧啶-7(8H)-酮 卡非佐米
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