达格列净的发现：一种用于治疗2型糖尿病的强效、选择性肾钠依赖性葡萄糖转运蛋白2（SGLT2）抑制剂。
Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.
作者信息
Meng Wei, Ellsworth Bruce A, Nirschl Alexandra A, McCann Peggy J, Patel Manorama, Girotra Ravindar N, Wu Gang, Sher Philip M, Morrison Eamonn P, Biller Scott A, Zahler Robert, Deshpande Prashant P, Pullockaran Annie, Hagan Deborah L, Morgan Nathan, Taylor Joseph R, Obermeier Mary T, Humphreys William G, Khanna Ashish, Discenza Lorell, Robertson James G, Wang Aiying, Han Songping, Wetterau John R, Janovitz Evan B, Flint Oliver P, Whaley Jean M, Washburn William N
机构信息
Drug Safety Evaluation and Development, Bristol -Myers Squibb Company, Princeton, New Jersey 08543, USA.
出版信息
J Med Chem. 2008 Mar 13;51(5):1145-9. doi: 10.1021/jm701272q. Epub 2008 Feb 9.
The C-aryl glucoside 6 (dapagliflozin) was identified as a potent and selective hSGLT2 inhibitor which reduced blood glucose levels in a dose-dependent manner by as much as 55% in hyperglycemic streptozotocin (STZ) rats. These findings, combined with a favorable ADME profile, have prompted clinical evaluation of dapagliflozin for the treatment of type 2 diabetes.
C-芳基葡萄糖苷6（达格列净）被鉴定为一种强效且选择性的人钠-葡萄糖协同转运蛋白2（hSGLT2）抑制剂，它能使高血糖链脲佐菌素（STZ）大鼠的血糖水平以剂量依赖的方式降低多达55%。这些发现，再加上良好的吸收、分布、代谢和排泄（ADME）特性，促使对达格列净进行治疗2型糖尿病的临床评估。
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