Cadisegliatin

Cadisegliatin (TTP-399) is a potential, orally active liver-selective glucokinase (GK) activator. Cadisegliatin has antihyperglycaemic activity. Cadisegliatin can be used for the research of type 2 diabetes. In Vitro Cadisegliatin (TTP-399) increases glucose metabolism in rat hepatocytes, the EC 50 values of lactate and glycogen in 15 nM glucose are 2.39 μM and 2.64 μM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo TTP399 (200 mg/kg, per os, p.o.) has no effect on plasma glucose and insulin in fasted rats. TTP399 (75 or 150 mg/kg, per day, for 4 weeks) improves glucose homeostasis in ob/ob mouse model. TTP399 (50 mg/kg, per day, for 13 weeks) is effective in reducing plasma glucose during an oral glucose tolerance test (OGTT) in minipigs model. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nondiabetic fasted ratsDosage: 200 mg/kg Administration: 200 mg/kg, per os (p.o.) Result: Did not change the insulin and glucose concentrations in plasma. Animal Model: ob/ob mouse modelDosage: 75 or 150 mg/kg Administration: 75 or 150 mg/kg, per day, for 4 weeks Result: Reduced the expression of HbA1c, blood glucose concentrations, lactate concentrations and liver glycogen depots. Improved the lipid profile, reduced plasma, liver TG concentrations and the weight gain at the highest dose. Animal Model: Gottingen minipigsDosage: 50 mg/kg Administration: 50 mg/kg, per day, for 13 weeks Result: Eliminated the blood glucose excursion in Minipigs. Form:Solid

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