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      GLPG0634 analogue
      GLPG0634 analogue

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V0328
      CAS #: 1206101-20-3Purity ≥98%

      Description: GLPG0634 analogue, an analog of Filgotinib (GLPG0634),  is a novel, potent and selective Janus kinase-JAK1 inhibitor with potential anti-inflammatory activity. It inhibits JAK1, JAK2, JAK3, and TYK2 with IC50s of 10, 28, 810, and 116 nM, respectively. It has the potential to be used for treating RA-rheumatoid arthritis. It dose-dependently reduces inflammation, cartilage, and bone degradation in the CIA model in rats and mice.

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

      Related CAS: 1206161-97-8 (Filgotinib / GLPG0634); 1206101-20-3;

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      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


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      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.

      These protocols are for reference only. InvivoChem does not independently validate these methods.

      GLPG0634 analogue

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

      GLPG0634 analogue

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

      GLPG0634 analogue

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

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