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GLPG0634 analogue
本半岛bd体育手机客户端 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。
GLPG0634 analogue图片
CAS NO:1206101-20-3
规格:≥98%
包装与价格：
包装价格(元)
5mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

半岛bd体育手机客户端 介绍
理化性质和储存条件
Molecular Weight (MW)410.43
FormulaC23H18N6O2
CAS No.1206101-20-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 0.1 mg/mL (0.24 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILESO=C(C1CC1)NC2=NN3C(C4=CC=C(OCC5=CC=C(C#N)N=C5)C=C4)=CC=CC3=N2
SynonymsFilgotinib-analogue; Filgotinib analogue, GLPG0634 analog; GLPG 0634 analogue; GLPG-0634 analogue; GLPG 0634 analogue
实验参考方法
In Vitro

In vitro activity: In cell lines, GLPG0634 inhibits IL-2- and IL-4-induced JAK1/JAK3/γc signaling and IFN-αB2-induced JAK1/TYK2 type II receptor signaling with IC50 ranged from 150 to 760 nM. GLPG0634 shows higher selectivity for JAK/STAT signaling involving JAK1 than JAK2 kinase in a cellular context. Besides, GLPG0634 also inhibits the differentiation of Th1, Th2, and Th17 cells.

Kinase Assay: GLPG0634 (analog) (compound176)is a pan JAK inhibitor with IC50s of 50-200 nM for JAK1/JAK2/JAK3; more information can be found in the reference patents.

In VivoFollowing oral administration, the absolute bioavailability was moderate in rats (45%) and high in mice (~100%). GLPG0634 (30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)) dose-dependently reduces inflammation, cartilage, and bone degradation in the CIA model in rats and mice.
Animal modelRat and mouse CIA model
Formulation & DosageDissolved in 0.5% (v/v) methylcellulose; 30 mg/kg (Rats) and 50 mg/kg (Mice); Oral administration
References

J Immunol. 2013 Oct 1;191(7):3568-77.

生物活性


GLPG0634 inhibits the differentiation of Th1, Th2, and Th17 cells. J Immunol.2013 Oct 1;191(7):3568-77.


GLPG0634 dose-dependently prevents disease progression in the therapeutic rat CIA model. J Immunol. 2013 Oct 1;191(7):3568-77.


GLPG0634 is efficacious in a mouse therapeutic CIA model. J Immunol. 2013 Oct 1;191(7):3568-77.

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