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「同位素标记抑制剂」Sitagliptin-d4 hydrochloride

发布时间:2025-06-12     作者:德尔塔生物   分享到:

【产品介绍】:

生物活性:Sitagliptin-d4 (hydrochloride) is the deuterium labeled Sitagliptin[1]. Sitagliptin (MK-0431) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[2].
体外研究(In Vitro):Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Sitagliptin-d4 hydrochloride 相关抗体:
DPP4/CD26 Antibody (YA1274)
分子量:447.80
Formula:C16H12D4ClF6N5O
非标记 CAS:486460-32-6
性状:固体
颜色:White to off-white
中文名称:西格列汀-d4;西他列汀-d4
运输条件:Room temperature in continental US; may vary elsewhere.
储存方式:4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
纯度 & 产品资料
纯度: 99.22%
参考文献
[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]. 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.
 [Content Brief]
[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.
 [Content Brief]
[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.
 [Content Brief]
[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.
 [Content Brief]
[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.
 [Content Brief]