1. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  2. JAK
  3. Filgotinib maleate

Filgotinib maleate  (Synonyms: GLPG0634 maleate)

Cat. No.: HY-18300A
Handling Instructions

Filgotinib (maleate) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM and 116 nM for JAK1, JAK2, JAK3 and TYK2, respectively. Filgotinib (maleate) can be used for rheumatoid arthritis (RA) and Crohn's disease research.

For research use only. We do not sell to patients.

Filgotinib maleate Chemical Structure

Filgotinib maleate Chemical Structure

CAS No. : 1802998-75-9

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Description

Filgotinib (maleate) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM and 116 nM for JAK1, JAK2, JAK3 and TYK2, respectively. Filgotinib (maleate) can be used for rheumatoid arthritis (RA) and Crohn's disease research[1][2].

IC50 & Target[1]

JAK1

10 nM (IC50)

JAK2

28 nM (IC50)

JAK3

810 nM (IC50)

Tyk2

116 nM (IC50)

In Vitro

Filgotinib (maleate) (1-10 μM) inhibits Th1 and Th2 differentiation in a dose-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Filgotinib (maleate) (1-10 mg/mL; p.o. and i.v.; Rat collagen-induced arthritis) exhibits good pharmacokinetic profiles and reduces paw swelling, bone and cartilage degradation and levels ofinflammatory cytokines[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rat collagen-induced arthritis (CIA)[1]
Dosage: 1 and 10 mg/kg
Administration: Oral administration; for 4 days
Result: Reduced infiltration of inflammatory cells while protecting the articular cartilage and bone.
Animal Model: Rat collagen-induced arthritis (CIA)[1]
Dosage: 1 and 5 mg/kg
Administration: Oral administration and intravenous injection
Result: 1.19
Parameter (Unit) Mouse 1 mg/kg i.v. Mouse 5 mg/kg Orally Rat 1 mg/kg i.v. Rat 5 mg/kg Orally
Cmax or Co (ng/mL) 637 920 1407 (28) 310 (33)
Tmax (h) 0.5 22 (0.5-5)
Area under curve:0-24 h (ng/h/mL) 347 1893 739 (2) 1681 (8)
T1/2 (h) 2.5 1.7 1.6 3.9
Cl (L/h/kg) 2.9 1.4
Vss (L/kg) 6 1.8
F (%)
Clinical Trial
Molecular Weight

541.58

Formula

C25H27N5O7S

CAS No.
SMILES

OC(/C=C\C(O)=O)=O.O=C(C1CC1)NC2=NN3C(C4=CC=C(C=C4)CN5CCS(=O)(CC5)=O)=CC=CC3=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Filgotinib maleate Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Filgotinib maleate
Cat. No.:
HY-18300A
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