5-Thiazolecarbonitrile, 2-[[2-ethyl-6-[4-[2-(3-hydroxy-1-azetidinyl)-2-oxoethyl]-1-piperazinyl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)-
2-((2-ethyl-6-(4-(2-(3-hydroxyazetidin-1-yl)-2-oxoethyl)piperazin-1-yl)-8-methylimidazo[1,2-a]pyridin-3-yl)(methyl)amino)-4-(4-fluorophenyl)thiazole-5-carbonitrile;ziritaxestat
CAS: 1628260-79-6
Molecular Formula: C30H33FN8O2S
5-Thiazolecarbonitrile, 2-[[2-ethyl-6-[4-[2-(3-hydroxy-1-azetidinyl)-2-oxoethyl]-1-piperazinyl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)- - Names and Identifiers
5-Thiazolecarbonitrile, 2-[[2-ethyl-6-[4-[2-(3-hydroxy-1-azetidinyl)-2-oxoethyl]-1-piperazinyl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)- - Physico-chemical Properties
| Molecular Formula | C30H33FN8O2S |
| Molar Mass | 588.6988232 |
| Density | 1.42±0.1 g/cm3(Predicted) |
| pKa | 13.72±0.20(Predicted) |
| Storage Condition | -20℃ |
| Physical and Chemical Properties | Bioactive Ziritaxestat (GLPG1690) is a selective autotoxin inhibitor with an IC50 of 131 nM and a Ki value of 15 nM. |
| Use | Introduction GLPG1690 is a selective autocrine motistatin found in Galapagos and may be used in idiopathic lung disease (IPF). In a phase 1 study of healthy human volunteers, GLPG1690 showed good safety and tolerability, as well as strong pharmacodynamic signals suggesting target involvement. |
5-Thiazolecarbonitrile, 2-[[2-ethyl-6-[4-[2-(3-hydroxy-1-azetidinyl)-2-oxoethyl]-1-piperazinyl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.699 ml | 8.493 ml | 16.987 ml |
| 5 mM | 0.34 ml | 1.699 ml | 3.397 ml |
| 10 mM | 0.17 ml | 0.849 ml | 1.699 ml |
| 5 mM | 0.034 ml | 0.17 ml | 0.34 ml |
Last Update：2024-01-02 23:10:35
5-Thiazolecarbonitrile, 2-[[2-ethyl-6-[4-[2-(3-hydroxy-1-azetidinyl)-2-oxoethyl]-1-piperazinyl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)- - Uses and synthesis methods
clinical study
The first small molecule Autotaxin(ATX, autocrine motility factor inhibitor) inhibitor Ziritaxestat(GLPG-1690) developed by the Belgian company Galapagos NV is currently undergoing phase III clinical trials for the treatment of idiopathic pulmonary fibrosis (IPF) or chronic obstructive pulmonary disease (COPD).
GLPG1690 is an investigational small molecule, selective autotaxin inhibitor. Autotaxin is the main enzyme that produces lysophosphatidic acid (LPA). LPA is a well-known pro-fibrotic and pro-inflammatory lipid. Galapagos company uses its proprietary target discovery platform to identify autotaxin targets and develop GLPG1690 molecules as inhibitors of the target. GLPG1690 is currently conducting a global phase 3 study for the treatment of idiopathic pulmonary fibrosis and a phase 2 NOVESA trial. The effectiveness and safety of the GLPG1690 have not been determined by any regulatory agency.
Target
Target Value
Autotaxin
15 nM(Ki)
Last Update：2024-04-09 21:01:54
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Spot supply
Product Name: GLPG-1690 Visit Supplier Webpage Request for quotationCAS: 1628260-79-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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