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Ziritaxestat

Catalog No. T4041 CAS 1628260-79-6

Synonyms: GLPG1690

Ziritaxestat (GLPG1690), an autotaxin inhibitor, currently being evaluated in an exploratory phase 2 study in idiopathic pulmonary fibrosis patients.

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Ziritaxestat, CAS 1628260-79-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 122.00
50 mg	In stock	$ 198.00
100 mg	In stock	$ 369.00
200 mg	In stock	$ 549.00
1 mL * 10 mM (in DMSO)	In stock	$ 56.00

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Purity: 99.67%

Purity: 97%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ziritaxestat (GLPG1690), an autotaxin inhibitor, currently being evaluated in an exploratory phase 2 study in idiopathic pulmonary fibrosis patients.
Targets&IC50	ATX:15 nM.
Kinase Assay	Glutaminase Inhibition: Cell Free Assay: Assay plates are prepared containing 2 μL test compound in DMSO/well. The enzyme is diluted to 1 unit (liver) or 0.8 unit (kidney)/100 μL in glutaminase assay buffer, and 100 μL diluted enzyme is added to each well of the assay plate by Multidrop. The contents are mixed by shaking at full speed for 1 min on TiterMix 100. The plates are preincubated at room temperature (RT) for 20 min to allow binding of test compounds to glutaminase, and 50 μL glutamine solution (7 mM in assay buffer) is added to each well by Multidrop. The contents are shaken at full speed for 30 sec on TiterMix 100, and the plates are then incubated at RT for 60 min (liver) or 90 min (kidney). To stop the reactions, 20 μL HCl (0.3 N) is added to each well by Multidrop and mixed immediately by shaking for 30 sec on TiterMix 100. For quantification, glutamate (formed by glutaminase-catalyzed hydrolysis of glutamine) is oxidized to 2-oxoglutarate by a second enzyme, glutamate dehydrogenase (GDH), with the concomitant production of the reduced form of nicotinamide adenine dinucleotide (NADH). Reduction of nitro blue tetrazolium (NBT) in the assay solution by NADH, catalyzed by phenazine methosulphate (PMS), results in the formation of a blue-purple formazan. The absorption of formazan at 540 nm is linearly proportional to the concentration of glutamate up to 200 μM. NBT/GDH reagent (50 μL) is added to each well by Multidrop and mixed by shaking for 30 sec on TiterMix 100, and the plates are incubated at RT for 20 min to allow color formation by the GDH reaction. Glutamate concentration is determined from formazan concentration as determined by reading OD540 nm on a SpectraMax 340.

Synonyms	GLPG1690
Molecular Weight	588.7
Formula	C30H33FN8O2S
CAS No.	1628260-79-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 0.1 mg/mL (insoluble)

DMSO: 41.67 mg/mL (70.78 mM), Sonification is recommended.

References and Literature

1. Desroy N., et al. Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinicalal Evaluation for the Treatment of Idiopathic PulmoN/Ary Fibrosis. J Med Chem. 2017 May 11;60(9):3580-3590. 2. Balupuri A., et al. Design, synthesis, docking and biological evaluation of 4-phenyl-thiazole derivatives as autotaxin (ATX) inhibitors. Bioorg Med Chem Lett. 2017 Jul 16. pii: S0960-894X(17)30718-7. 3. Chen J, Guan Z, Dong N, et al. A novel LC–MS/MS method for the determination of ziritaxestat in rat plasma and its pharmacokinetic study[J]. Biomedical Chromatography. 2020: e4863. 4. Chen J, Guan Z, Dong N, et al. A novel LC‐MS/MS method for the determination of ziritaxestat in rat plasma and its pharmacokinetic study[J]. Biomedical Chromatography. 2020: e4863. 5. Yang Y, Zhang X, Zhang X, et al. Modulators of histone demethylase JMJD1C selectively target leukemic stem cells[J]. FEBS Open Bio. 2020

Citations

1. Yang Y, Zhang X, Zhang X, et al. Modulators of histone demethylase JMJD1C selectively target leukemic stem cells. FEBS Open Bio. 2020 2. Chen J, Guan Z, Dong N, et al. A novel LC‐MS/MS method for the determination of ziritaxestat in rat plasma and its pharmacokinetic study. Biomedical Chromatography. 2020: e4863. 3. Hu Y, Li L, Tian Y, et al.Design, synthesis and evaluation of novel UDCA-aminopyrimidine hybrids as ATX inhibitors for the treatment of hepatic and pulmonary fibrosis.European Journal of Medicinal Chemistry.2023: 116029.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library Inhibitor Library ReFRAME Related Library Anti-Fibrosis Compound Library Bioactive Compounds Library Max Fluorochemical Library Bioactive Compound Library Clinical Compound Library Anti-Metabolism Disease Compound Library

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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.

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Keywords

Ziritaxestat 1628260-79-6 Metabolism PDE Inhibitor GLPG-1690 GLPG1690 GLPG 1690 inhibit Phosphodiesterase (PDE) inhibitor

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