SJ-MX2873
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AR 231453
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AR 231453 is a potent and orally active agonist of cannabinoid receptor GPR119.
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SJ-MX3263
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MBX-2982
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MBX-2982 is a potent and selective agonist of G-protein coupled receptor 119 (GPR119); an orally active agent to treat type 2 diabetes; MBX 2982 acts directly on the β cell to increase insulin secretion. In addition, it stimulates release of the incretin GLP-1 from the gut
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SJ-MX2993
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APD668
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APD668 is a potent and selective, orally active G protein-coupled receptor 119 agonist (EC50 values 2.7 nM and 23 nM for hGPR119 and rGPR119, respectively) with in vivo activity in rodent models of glucose control. APD 668 significantly improved blood glucose handling during glucose challenge in several diabetic and non-diabetic rodent models, showing a clear glucose-dependent effect on insulin release in a hyperglycemic clamp model in the Sprague–Dawley rat. APD 668 is not genotoxic, and shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki value 0.1 μM).
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SJ-MX2126
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GSK-1292263
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GSK-1292263 是一种有效的,具有口服活性的 GPR119 激动剂,作用于人和大鼠 GPR119,pEC50 分别为 6.9 和 6.7。GSK-1292263 可用于 2 型糖尿病 (T2DM) 的研究。
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SJ-MX1170
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AS1269574
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AS1269574 是一种有效的,具有口服活性的 GPR119 激动剂,在表达人 GPR119 的 HEK293 细胞中 EC50 为 2.5 μM。AS1269574 激活 TRPA1 阳离子通道,刺激胰高血糖素样肽-1 (GLP-1) 分泌。AS1269574 仅在高糖条件下特异性诱导胰腺β 细胞分泌葡萄糖依赖性胰岛素。AS1269574 对 2 型糖尿病研究具有潜力。
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SJ-MX5512
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APD597
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