Trelagliptin-13C,d3,2707203-34

Trelagliptin-13C,d3 产品活性：Trelagliptin-13C,d3是氘代标记的Trelagliptin。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。 产品来源： www.medchemexpress.cn/trelagliptin-13c-d3.html 研究领域：Others | Metabolic Enzyme/Protease 作用靶点：Isotope-Labeled Compounds | Dipeptidyl Peptidase In Vitro: Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.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. 相关产品：Sitagliptin | Talabostat mesylate | Puromycin aminonucleoside | Linagliptin | Brensocatib | Saxagliptin | Vildagliptin | Omarigliptin | 1G244 | Diprotin A | L-Lactic acid-13C3 sodium | L-Valine-d8 | Sodium cyanoboronhydride-d3 | Nateglinide | 3-Indoleacetic acid-d5 | Teneligliptin | Alogliptin | Water-18O | Kynurenic acid-d5 | Retinol-d5 | Trelagliptin | Gemigliptin tartrate | Inosine-13C5 | Anagliptin 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前沿最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TOP期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪前沿的制药及生命科学研究进展，为您提供全球前沿的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。