Linagliptin-13C,d3(Synonyms: BI 1356-13C,d3)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物,专注于信号通路和疾病研究领域。
Linagliptin-13C,d3 (Synonyms: BI 1356-13C,d3)

Linagliptin-13C,d3 是一种 13C- 和氘代标记的 Linagliptin。Linagliptin 是一种有效,选择性的 DPP-4 抑制剂,IC50 值为 1 nM。

Linagliptin-13C,d3(Synonyms: BI 1356-13C,d3)

Linagliptin-13C,d3 Chemical Structure

CAS No. : 1398044-43-3

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生物活性

Linagliptin-13C,d3 is the 13C- and deuterium labeled. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.

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[82].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

476.55

Formula

C2413CH25D3N8O2

CAS 号

1398044-43-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献
  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223.

    [2]. Eckhardt M, et al. 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 d

    [3]. 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

    [4]. Schurmann C, et al. The dipeptidyl peptidase-4 inhibitor linagliptin attenuates inflammation and accelerates epithelialization in wounds of diabetic ob/ob mice. J Pharmacol Exp Ther. 2012 Jul;342(1):71-80.

    [5]. Huan Y, et al. The dual DPP4 inhibitor and GPR119 agonist HBK001 regulates glycemic control and beta cell function ex and in vivo. Sci Rep. 2017 Jun 28;7(1):4351.

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