Ziritaxestat (GLPG1690)

Catalog No.S8895

For research use only.

Ziritaxestat (GLPG1690) is a selective autotaxin inhibitor with an IC50 of 131 nM and Ki of 15 nM.

Ziritaxestat (GLPG1690) Chemical Structure

CAS No. 1628260-79-6

Selleck's Ziritaxestat (GLPG1690) has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description Ziritaxestat (GLPG1690) is a selective autotaxin inhibitor with an IC50 of 131 nM and Ki of 15 nM.
Targets
Autotaxin [1]
15 nM(Ki)
Assay
Methods Test Index PMID
Clinical Recovery Lysophosphatidic Acid (LPA) 30953319
In vivo

Ziritaxestat (GLPG1690) decreases LPA levels in a sustainable manner, in mouse plasma, from a dose of 3 mg/kg onward. It demonstrates significant activity in the mouse BLM-induced fibrosis model at doses of 10 and 30 mg/kg twice a day[1].

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: Female C57BL/6Rj mice, 4-5 weeks old
  • Dosages: 3, 10, or 30 mg/kg
  • Administration: oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 588.70
Formula

C30H33FN8O2S

CAS No. 1628260-79-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1=C(N2C=C(C=C(C2=N1)C)N3CCN(CC3)CC(=O)N4CC(C4)O)N(C)C5=NC(=C(S5)C#N)C6=CC=C(C=C6)F

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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
NCT03515382 Completed Drug: GLPG1690|Drug: Itraconazole|Drug: Voriconazole Healthy Galapagos NV March 16 2018 Phase 1
NCT03143712 Completed Drug: GLPG1690 Healthy Galapagos NV April 18 2017 Phase 1
NCT02738801 Completed Drug: GLPG1690 600 mg QD|Drug: Placebo QD Idiopathic Pulmonary Fibrosis Galapagos NV March 2016 Phase 2

(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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