Baricitinib-d5(Synonyms: LY3009104-d5; INCB028050-d5)

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Baricitinib-d5 (Synonyms: LY3009104-d5; INCB028050-d5)

Baricitinib-d5 (LY3009104-d5) 是 Baricitinib 的氘代物。Baricitinib (LY3009104; INCB028050) 是选择性，可口服的 JAK1 和 JAK2 抑制剂，IC50 分别为5.9 nM 和 5.7 nM。

Baricitinib-d5(Synonyms: LY3009104-d5; INCB028050-d5)

Baricitinib-d5 Chemical Structure

CAS No. : 1564241-79-7

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生物活性

Baricitinib-d5 (LY3009104-d5) is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.

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].

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

376.45

Formula

C16H12D5N7O2S
CAS 号

1564241-79-7
中文名称

巴瑞克替尼 d5
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):211-216.

    [2]. Fridman JS, et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol. 2010 May 1;184(9):5298-307.

    [3]. Jabbari A, et al. Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib. EBioMedicine. 2015 Feb 26;2(4):351-5.

    [4]. Khan IM, et al. Intermuscular and perimuscular fat expansion in obesity correlates with skeletal muscle T cell and macrophage infiltration resistance. Int J Obes (Lond). 2015 Nov;39(11):1607-18.

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