Trelagliptin曲格列汀,865759-25-7

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Trelagliptin

CAS No. : 865759-25-7

MCE 国际站：Trelagliptin

产品活性：Trelagliptin (SYR-472) 是一种有效的，具有口服活性 DPP-4 抑制剂，IC₅₀ 为 4 nM。Trelagliptin (SYR-472) 改善体内血糖控制，可用于2 型糖尿病 (T2DM) 的研究。

研究领域：Metabolic Enzyme/Protease

作用靶点：Dipeptidyl Peptidase

In Vitro: Dipeptidyl peptidase-4 (DPP-4) is one of the widely explored novel targets for type 2 diabetes mellitus (T2DM) strategy to preserve the endogenous glucagon like peptide (GLP)-1 activity by inhibiting the DPP-4 action.
Trelagliptin exhibits potent inhibitory activity toward DPP-4 prepared from Caco-2 cells with an IC₅₀ value of 5.4 nM. Trelagliptin also inhibits human, dog, and rat plasma DPP-4 activity with IC₅₀ values of 4.2 nM, 6.2 nM, and 9.7 nM, respectively.
Trelagliptin is highly selective for DPP-4 and displays IC₅₀ values >100,000 nM corresponding to >10,000-fold selectivity over DPP-2, DPP-8, DPP-9, PEP and FAPα activities. Trelagliptin shows DPP4 selective about 4- and 12-fold more potent than alogliptin (HY-A0023) and sitagliptin (HY-13749), respectively.

In Vivo: Trelagliptin (oral gavage; 7 mg/kg; single dose) shows sustained PD effect in dogs and gives >80% inhibition of DPP-4 activity even after 24h.
Trelagliptin (oral gavage; 3 mg/kg; single dose; 60 min prior to oral glucose) significantly improves the glucose tolerance capacity by decreasing the AUC_0−120min of 19.3% compared with the vehicle group in ob/ob mice.
Trelagliptin (oral gavage; 10 mg/kg; once a week; 8 weeks) caused significant reductions in fasting blood glucose (FBG) levels, and the average reduction during the entire treatment period is 16.8% compared to the control.It also increases insulin level and raised it by 1.7-foldin AUC_0−120min in ob/ob mice.

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