GLPG0634 analogue

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GLPG0634 analogue

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。

CAS NO:	1206101-20-3
规格:	≥98%

包装与价格：

产品介绍

理化性质和储存条件

Molecular Weight (MW)	410.43
Formula	C23H18N6O2
CAS No.	1206101-20-3
Storage	-20℃ for 3 years in powder form
Storage	-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
SMILES	O=C(C1CC1)NC2=NN3C(C4=CC=C(OCC5=CC=C(C#N)N=C5)C=C4)=CC=CC3=N2
Synonyms	Filgotinib-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 Vivo	Following 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 model	Rat and mouse CIA model
Formulation & Dosage	Dissolved 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.