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Filgotinib-d4
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Filgotinib-d4图片
CAS NO:2041095-50-3
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
Filgotinib-d4 (GLPG0634-d4) 是氘标记的 Filgotinib。 Filgotinib (GLPG0634) 是一种选择性 JAK1 抑制剂，对 JAK1、JAK2、JAK3 和 TYK2 的 IC50 分别为 10 nM、28 nM、810 nM 和 116 nM。
Cas No.2041095-50-3
别名GLPG0634-d4
Canonical SMILESO=S1(CCN(CC2=CC=C(C3=CC=CC4=NC(NC(C5C([2H])([2H])C5([2H])[2H])=O)=NN43)C=C2)CC1)=O
分子式C21H19D4N5O3S
分子量429.5
溶解度Acetonitrile:Methanol (1:1): soluble,DMSO: soluble
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Filgotinib-d4 is intended for use as an internal standard for the quantification of filgotinib by GC- or LC-MS. Filgotinib is a JAK1 inhibitor (IC50 = 10 nM).1 It is selective for JAK1 over JAK3 (IC50 = 810 nM) but also inhibits JAK2 and tyrosine kinase 2 (Tyk2; IC50s = 28 and 116 nM, respectively), as well as Abl, FLT1, -3 and -4, FMS, Mer, and TBK1 activity by greater than 35% in a panel of 177 tyrosine kinases at 1 μM. Filgotinib inhibits IL-6-induced phosphorylation of STAT1 in CD4+ T cells with an IC50 value of 629 nM in isolated human whole blood. It reduces hind paw macrophage and T cell infiltration and bone erosion in a rat model of collagen-induced arthritis when administered at doses ranging from 0.1 to 30 mg/kg per day for 15 days.

|1. Van Rompaey, L., Galien, R., van der Aar, E.M., et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J. Immunol. 191(7), 3568-3577 (2013).