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MedChemExpress - Model Filgotinib - ...

MedChemExpress - Model Filgotinib - 1206161-97-8

Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease[1][2][3].

Filgotinib

MCE China：Filgotinib

Brand：MedChemExpress (MCE)

Cat. No.HY-18300

CAS：1206161-97-8

Synonyms：GLPG0634

Purity：99.44%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease.

In Vitro：Filgotinib (0.1, 1 and 10 μM) inhibits the differentiation of Th2 cells and Th1 cells in a dose-dependent manner[1].

In Vivo：Filgotinib (0.1, 0.3, 1, 3, 10 and 30 mg/kg, i.g.; once daily for 15 days) produces dose-dependent bone damage protection and prevents the development of inflammation in a rat model of collagen-induced arthritis[1]. Pharmacokinetic analysis of GLPG0634 in mice[1] Route Dose (mg/kg) C0 or C0 (ng/mL) Tmax (h) T1/2 (h) Cl (L•h/kg) Vss (L/kg) F (%) i.v. 1 637 / 2.5 2.9 6 / p.o. 5 920 0.5 1.7 / / 100 Pharmacokinetic analysis of GLPG0634 in rats[1] Route Dose (mg/kg) C0 or C0 (ng/mL) Tmax (h) T1/2 (h) Cl (L•h/kg) Vss (L/kg) F (%) i.v. 1 1407 / 1.6 1.4 1.8 / p.o. 5 310 2.2 3.9 / / 45

IC50 & Target：JAK1 10 nM (IC50) JAK2 28 nM (IC50) Tyk2 116 nM (IC50) JAK3 810 nM (IC50)

References：

[1]. Van Rompaey L, et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol. 2013, 191(7), 3568-3577. [Content Brief]

[2]. Menet CJ, et al. Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634. J Med Chem. 2014 Nov 17. [Content Brief]

[3]. Yeh, et al. "Filgotinib suppresses HIV-1–driven gene transcription by inhibiting HIV-1 splicing and T cell activation." The Journal of Clinical Investigation 130.9 (2020): 4969-4984. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。