MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Trelagliptin

CAS No. : 865759-25-7

MCE 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.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  FDA-Approved Drug Library  |  Drug Repurposing Compound Library  |  Diabetes Related Compound Library  |  Ferroptosis Compound Library  |  Anti-COVID-19 Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Talabostat mesylate  |  Puromycin aminonucleoside  |  Vildagliptin  |  1G244  |  Diprotin A TFA  |  Nateglinide  |  Prolyl Endopeptidase Inhibitor 1  |  DPP-IV-IN-2  |  Prodipine hydrochloride  |  Saikogenin A  |  UAMC00039 dihydrochloride  |  2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one  |  Azaleatin  |  Evogliptin tartrate  |  NDMC101  |  NVP-DPP728 dihydrochloride  |  DPP-IV-IN-1

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。