Ertugliflozin-d₉  (Synonyms: 埃格列净-d₉; PF-04971729-d₉)

Ertugliflozin-d₉ is deuterated labeled Ertugliflozin (HY-15461). Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC₅₀ of 0.877 nM for h-SGLT2^[1]. Has the potential for the treatment of type 2 diabetes mellitus^[2].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
Ertugliflozin (PF-04971729) 在体外对 SGLT2 抑制 (相对于 SGLT1) 表现出 >2000 倍的选择性^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Ertugliflozin (PF-04971729) 在大鼠口服给药后表现出浓度依赖性糖尿^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

445.94

C₂₂H₁₆D₉ClO₇

1210344-57-2

埃格列净-d₉

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Mascitti V, et al. Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. J Med Chem. 2011 Apr 28;54(8):2952-60.  [Content Brief]

  [3]. Miao Z, et al. Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos. 2013 Feb;41(2):445-56.  [Content Brief]

  [4]. Kalgutkar AS, et al. Preclinical species and human disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus. Drug Metab Dispos. 2011 Sep;39(9):1609-19.  [Content Brief]