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TAK-875 (CAS 1000413-72-8) is a selective orally bioavailable agonist targeting G-protein-coupled receptor 40 (GPR40) a receptor primarily expressed in pancreatic -cells Activation of GPR40 enhances glucose-dependent insulin secretion via free fatty acid signaling In vitro assays demonstrate that TAK-875 exhibits potent agonistic activity toward human GPR40 with minimal cross-reactivity against other related receptors in the free fatty acid receptor family (EC50 10 M) Additionally in vivo studies in glucose-intolerant obese Wistar rats have shown that oral administration of TAK-875 improves glucose tolerance and stimulates insulin release Clinically TAK-875 has been explored as a glucose-dependent insulin secretagogue with once-daily oral dosing potential
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