rac-Sitagliptin-d4 hydrochloride

rac-Sitagliptin-d4 hydrochloride用途

(Rac)-西他列汀-d4((Rac)-MK-0431-d4)盐酸盐是一种标记的外消旋西他列汀。盐酸西他列汀(MK-0431)是DPP4的有效抑制剂,在Caco-2细胞提取物中的IC50为19 nM[1]。

rac-Sitagliptin-d4 hydrochloride名称

[ CAS 号 ]:
1620233-77-3

[ 英文名 ]:
rac-Sitagliptin-d4 hydrochloride

rac-Sitagliptin-d4 hydrochloride生物活性

[ 描述 ]:

(Rac)-西他列汀-d4((Rac)-MK-0431-d4)盐酸盐是一种标记的外消旋西他列汀。盐酸西他列汀(MK-0431)是DPP4的有效抑制剂,在Caco-2细胞提取物中的IC50为19 nM[1]。

[ 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-ylmethyl)-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 action compared with other dipeptidyl peptidase-4 inhibitors. J Pharmacol Exp Ther. 2008 Apr;325(1):175-82.

[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 GLP-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.

rac-Sitagliptin-d4 hydrochloride物理化学性质

[ 分子式 ]:
C₁₆H₁₂D₄ClF₆N₅O

[ 分子量 ]:
411.34

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相关化合物

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标题：【rac-Sitagliptin-d4 hydrochloride】rac-Sitagliptin-d4 hydrochloride CAS号:1620233-77-3【结构式性质活性】-化源网地址：https://www.chemsrc.com/amp/cas/1620233-77-3_1682354.html