Trelagliptin succinate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Trelagliptin (SYR-472) 是一种长效二肽基肽酶 4 (DPP-4) 抑制剂，开发用于治疗 2 型糖尿病 (T2D)。

Trelagliptin(SYR-472) is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D).(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 AUC0?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-fold in AUC0?120min in ob/ob mice.

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 withIC50?values of 4.2 nM, 6.2 nM, and 9.7 nM, respectively.Trelagliptin is highly selective for DPP-4 and displaysIC50?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.

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 AUC0?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-fold in AUC0?120min in ob/ob mice. Animal Model:ICR ob/ob mice Dosage:10 mg/kg Administration:Oral gavage; 10 mg/kg; once a week; 8 weeks Result:Exerted chronic antidiabetic effects on type 2 diabetic db/db Mice.

SYR-472

Metabolic Enzyme/Protease

DPP

DPP-4

Metabolic Disease

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1029877-94-8

475.47

C22H26FN5O6

>98% (HPLC)

DMSO: 10 mM

CN1C(=O)C=C(N(C1=O)CC2=C(C=CC(=C2)F)C#N)N3CCC[C@H](C3)N.C(CC(=O)O)C(=O)O

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(-20℃)

With Ice Pack

≥ 2 years