产品
编 号：F013714
分子式：C22H26FN5O6
分子量：475.47
分子式：C22H26FN5O6
分子量：475.47
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
400
In-stock
10mg
640
In-stock
50mg
960
In-stock
100mg
1280
In-stock
结构图
CAS No: 1029877-94-8
产品详情
生物活性：
Trelagliptin (SYR-472) succinate is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM).
体内研究：
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-foldin 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.
体外研究：
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 (SYR-472) succinate is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM).
体内研究：
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-foldin 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.
体外研究：
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.
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