Filgotinib-d4(Synonyms: GLPG0634-d4)

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Filgotinib-d4 (Synonyms: GLPG0634-d4)

Filgotinib-d4 (GLPG0634-d4) 是 Filgotinib 的氘代物。Filgotinib (GLPG0634) 是一种选择性的 JAK 抑制剂,能够有效抑制 JAK1,JAK2,JAK3 和 TYK2 的活性,IC50 值分别为 10 nM,28 nM,810 nM 和 116 nM。

Filgotinib-d4(Synonyms: GLPG0634-d4)

Filgotinib-d4 Chemical Structure

CAS No. : 2041095-50-3

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生物活性

Filgotinib-d4 (GLPG0634-d4) is the deuterium labeled Filgotinib. Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, 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

429.53

Formula

C21H19D4N5O3S

CAS 号

2041095-50-3

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):211-216.

    [2]. Van Rompaey L, et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol. 2013, 191(7), 3568-3577.

    [3]. Menet CJ, et al. Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634. J Med Chem. 2014 Nov 17.

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