Home Metabolism PDE inhibitor Ziritaxestat (GLPG1690) For research use only.

Ziritaxestat (GLPG1690)

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

Ziritaxestat (GLPG1690) Chemical Structure

Ziritaxestat (GLPG1690) Chemical Structure

CAS No. 1628260-79-6

Purity & Quality Control

Batch: S889501 DMSO]100 mg/mL]false]Ethanol]4 mg/mL]false]Water]Insoluble]false Purity: 99.48%
99.48

Ziritaxestat (GLPG1690) Related Products

Signaling Pathway

PDE Signaling Pathways

PDE Signaling Pathway

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)
In Vivo
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].
Animal Research Animal Models Female C57BL/6Rj mice, 4-5 weeks old
Dosages 3, 10, or 30 mg/kg
Administration oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03515382 Completed
Healthy
Galapagos NV
 March 16 2018 Phase 1
NCT03143712 Completed
Healthy
Galapagos NV
 April 18 2017 Phase 1
NCT02738801 Completed
Idiopathic Pulmonary Fibrosis
Galapagos NV
 March 2016 Phase 2

Chemical Information & Solubility

Molecular Weight 588.70 Formula

C30H33FN8O2S
CAS No. 1628260-79-6 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (169.86 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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In vivo Formulation Calculator

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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.
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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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