GLPG0634 analogue

Catalog No.S7137

For research use only.

GLPG0634 analogue 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.

GLPG0634 analogue Chemical Structure

CAS No. 1206101-20-3

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Biological Activity

Description GLPG0634 analogue 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.
Targets
JAK [1]
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. [1]

In vivo Following 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. [1]

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: Rat CIA model and mouse CIA model
  • Dosages: 30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 410.43
Formula

C23H18N6O2

CAS No. 1206101-20-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC1C(=O)NC2=NN3C(=N2)C=CC=C3C4=CC=C(C=C4)CN5CCS(=O)(=O)CC5

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02048618 Completed Drug: GLPG0634|Drug: Placebo Crohn''s Disease Galapagos NV February 2014 Phase 2
NCT01820806 Completed Drug: 100 mg dose of [14C] GLPG0634 Healthy Galapagos NV March 2013 Phase 1
NCT01798979 Completed Drug: GLPG0634|Drug: Midazolam Healthy Galapagos NV February 2013 Phase 1
NCT01665924 Completed Drug: GLPG0634 100mg capsule once a day for 10 days Healthy Galapagos NV July 2012 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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