Sitagliptin-d4 phosphate

• 常用名: Sitagliptin-d4 phosphate
• 英文名: Sitagliptin-d4 phosphate
• CAS号: 1432063-88-1
• 分子量: 509.33
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₆H₁₄D₄F₆N₅O₅P
• 熔点: N/A
• 闪点: N/A

Sitagliptin-d4 phosphate用途

西他列汀-d4(MK-0431-d4)磷酸盐是氘标记的西他列汀磷酸盐。西他列汀磷酸盐(MK-0431磷酸盐)是一种有效的DPP4抑制剂,在Caco-2细胞提取物中的IC50为19 nM[1][2]。

Sitagliptin-d4 phosphate名称

• 中文名: 西格列汀-d4磷酸盐
• 英文名: Sitagliptin-d4 phosphate

Sitagliptin-d4 phosphate生物活性

• 描述: 西他列汀-d4(MK-0431-d4)磷酸盐是氘标记的西他列汀磷酸盐。西他列汀磷酸盐(MK-0431磷酸盐)是一种有效的DPP4抑制剂,在Caco-2细胞提取物中的IC50为19 nM[1][2]。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 二肽基肽酶
  信号通路 >> 自噬 >> 自噬
  研究领域 >> 代谢疾病
• 体外研究: 氢、碳和其他元素的稳定重同位素已被纳入药物分子,主要作为药物开发过程中定量的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而受到关注[1]。
• 参考文献:

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

  [2]. Thomas, L., et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylm ethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of acti

  [3]. Kim, S.J., et al., Dipeptidyl peptidase IV inhibition with MK0431 improves islet graft survival in diabetic NOD mice partially via T-cell modulation. Diabetes, 2009. 58(3): p. 641-51.

  [4]. Sangle, G.V., et al., Novel biological action of the dipeptidylpeptidase-IV inhibitor, sitagliptin, as a glucagon-like peptide-1 secretagogue. Endocrinology, 2012. 153(2): p. 564-73.

  [5]. Kim, S.J., et al., Inhibition of dipeptidyl peptidase IV with sitagliptin (MK0431) prolongs islet graft survival in streptozotocin-induced diabetic mice. Diabetes, 2008. 57(5): p. 1331-9.

  [6]. Beconi, M.G., et al. Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs. Drug Metab Dispos, 2007. 35(4): p. 525-32.

Sitagliptin-d4 phosphate物理化学性质

• 分子式: C₁₆H₁₄D₄F₆N₅O₅P
• 分子量: 509.33
• 储存条件: -20°C