GPLG0634
| Price | $7 |
| Package | 1KG |
| Min. Order: | 1KG |
| Supply Ability: | JD 484 |
| Update Time: | 2019-09-02 |
Product Details
| Product Name: GPLG0634 | CAS No.: 1206161-97-8 |
| 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.
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;
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$7.00 / 1KG
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China- Since: 2014-12-17
- Address: No.967,15th Floor,Unit 7, Building 1, No.70 of DianChang Road, High-tech Development Zone, Zhengzho
INQUIRY
楊俊青
sales@coreychem.com
sales@coreychem.com