2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Anti-infection
  3. JAK HIV
  4. Filgotinib maleate

Filgotinib maleate  (Synonyms: GLPG0634 maleate)

Cat. No.: HY-18300A Purity: 99.88%
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Filgotinib maleate (GLPG0634 maleate) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib maleate 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 maleate also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib maleate can be used in the study of rheumatoid arthritis and inflammatory bowel disease.

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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Based on 17 publication(s) in Google Scholar

Other Forms of Filgotinib maleate:

Filgotinib maleate Related Antibodies

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JAK1 JAK2 JAK3 Tyk2 JAK

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  • Biological Activity

  • Purity & Documentation

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Description

Filgotinib maleate (GLPG0634 maleate) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib maleate 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 maleate also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib maleate can be used in the study of rheumatoid arthritis and inflammatory bowel disease[1][2][3].

IC50 & Target[1]

JAK1

10 nM (IC50)

JAK2

28 nM (IC50)

JAK3

810 nM (IC50)

Tyk2

116 nM (IC50)

In Vitro

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

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

Filgotinib maleate Related Antibodies
In Vivo

Filgotinib maleate (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

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

Animal Model: therapeutic rat CIA model[1]
Dosage: 0.1, 0.3, 1, 3, 10 and 30 mg/kg
Administration: i.g. 1 time per day for 15 days
Result: Reduced inflammatory cell infiltration while protecting articular cartilage and bone at a dose of 1 mg/kg.
Reduced serum levels of inflammatory cytokines and chemokines including IL-6, IP-10, XCL1, and MCP-1.
Clinical Trial
Molecular Weight

541.58

Formula

C25H27N5O7S
CAS No.
Appearance

Solid

Color

White to off-white

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 35 mg/mL (64.63 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8464 mL 9.2322 mL 18.4645 mL
5 mM 0.3693 mL 1.8464 mL 3.6929 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8464 mL 9.2322 mL 18.4645 mL 46.1612 mL
5 mM 0.3693 mL 1.8464 mL 3.6929 mL 9.2322 mL
10 mM 0.1846 mL 0.9232 mL 1.8464 mL 4.6161 mL
15 mM 0.1231 mL 0.6155 mL 1.2310 mL 3.0774 mL
20 mM 0.0923 mL 0.4616 mL 0.9232 mL 2.3081 mL
25 mM 0.0739 mL 0.3693 mL 0.7386 mL 1.8464 mL
30 mM 0.0615 mL 0.3077 mL 0.6155 mL 1.5387 mL
40 mM 0.0462 mL 0.2308 mL 0.4616 mL 1.1540 mL
50 mM 0.0369 mL 0.1846 mL 0.3693 mL 0.9232 mL
60 mM 0.0308 mL 0.1539 mL 0.3077 mL 0.7694 mL
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Filgotinib maleate Related Classifications

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.

Keywords:

Filgotinib1802998-75-9GLPG0634GLPG 0634GLPG-0634JAKHIVJanus kinaseHuman immunodeficiency virusrheumatoid arthritisCrohn's diseaseInhibitorinhibitorinhibit

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