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。

Gosogliptin

CAS No. : 869490-23-3

MCE 国际站：Gosogliptin

产品活性：Gosogliptin 是一种有效的选择性二肽基肽酶IV (DPP-IV) 抑制剂。

研究领域：Metabolic Enzyme/Protease

作用靶点：Dipeptidyl Peptidase

In Vitro: Gosogliptin (PF-00734200) is a potent, orally active, selective, and competitive inhibitor of DPP-IV, the enzyme mainly responsible for the degradation of the incretin peptides GLP-1 and glucose-dependent insulinotropic polypeptide. Gosogliptin demonstrates greater than 200-fold selectivity over other members of the DPP family (DPP-2, DPP-3, DPP-8, and DPP-9) and the related serine proteases, fibroblast activation protein, aminopeptidase P, and propyl oligopeptidase, enzymes that possess similar catalytic activities. Gosogliptin demonstrates rapid and reversible inhibition of plasma DPP-4 activity when administered orally to rats, dogs, and monkeys. In various nonclinical models, Gosogliptin stimulates insulin secretion and improves glucose tolerance.

In Vivo: The objectives of the present study are to characterize the metabolism, pharmacokinetics, and excretion of [¹⁴C] Gosogliptin in Sprague-Dawley (SD) rats, beagle dogs, and humans. A single dose of [¹⁴C] Gosogliptin is administered orally to intact SD rats (5 mg/kg), beagle dogs (5 mg/kg), and humans (20 mg). After a single oral dose of [¹⁴C] Gosogliptin to SD rats, an overall mean of 97.1% of the administered radioactivity is recovered in the urine, feces, and cage wash over a period of 168 h postdose. The mean cumulative dose recovered in feces is 66.0%. The mean cumulative excretion in the urine is 30.8%. Approximately 95% of the excreted radioactivity recovery occurred in the first 48 h. Mean total recoveries of dosed radioactivity from bile duct-cannulated rats are 29.5% in urine and 62.0% in bile. No gender-related differences are observed in the excretion pattern of radioactivity.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  NVP-DPP728  |  Gemigliptin  |  DPP IV/hCA II-IN-1  |  Linagliptin-d₄  |  HAEGT  |  Ellipyrone A  |  2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one  |  Anagliptin hydrochloride  |  Sitagliptin phosphate  |  P32/98  |  Vildagliptin-d₇  |  Dutogliptin  |  Prodipine hydrochloride  |  Teneligliptin-d₄  |  Nateglinide  |  DPP-4-IN-1  |  DBPR108  |  Sitagliptin fenilalanil hydrochloride  |  Teneligliptin  |  UAMC00039 dihydrochloride  |  Sheng Gelieting  |  Puromycin aminonucleoside  |  16-Hydroxycleroda-3,13-dien-15,16-olide  |  Talabostat isomer mesylate

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，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；
•   50,000 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；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   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 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。