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ChemicalBook Product Catalog Biochemical Engineering Inhibitors Protein tyrosine kinase /JAK / STAT JAK inhibitors GPLG0634

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GPLG0634

$ 7.00 /1KG

Min. Order1KG
Purity99%
Cas No1206161-97-8
Supply AbilityJD 484
Update time2019-09-02

career henan chemical co

6YR

China

Since2014-12-17

Address No.967,15th Floor,Unit 7, Building 1, No.70 of DianChang Road, High-tech Development Zone, Zhengzho

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Chemical Properties

Product Name	GPLG0634
CAS No	1206161-97-8
EC-No
Min. Order	1KG
Purity	99%
Supply Ability	JD 484
Release date	2019/09/02

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Product Name:

GPLG0634

Synonyms:

1206161-97-8;GPLG0634;GLPG0634;SYN1158;CyclopropanecarboxaMide, N-[5-[4-[(1,1-dioxido-4-thioMorpholinyl)Methyl]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]-;GLPG0634 (analog);N-[5-[4-[(1,1-Dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide;Filgotinib (GLPG0634)

CAS:

1206161-97-8

MF:

C21H23N5O3S

MW:

425.51

EINECS:

Product Categories:

API;Inhibitors;-

Mol File:

1206161-97-8.mol

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GPLG0634 Chemical Properties

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Safety Information

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MSDS Information

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GPLG0634 Usage And Synthesis

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Description

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. Phase 2.

In vitro

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.

In vivo

Following oral administration, the absolute bioavailability is moderate in rats (45%) and high in mice (～100%). Filgotinib (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. Filgotinib (GLPG0634) in DSS-treated mice demonstrates that inhibition of JAK1 is sufficient for achieving strong efficacy in pre-clinical mouse model, correlated to the inhibition of STAT3 phosphorylation in the inflamed colon.

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Company Profile Introduction

Established in 2014,Career Henan Chemical Co. is a manufacturerspecializing in the sale of fine chemicals. Mainly deals in the sales of: Pharmaceutical intermediates OLED intermediates： Pharmaceutical intermediates; OLED intermediates;