GLPG-1690
GLPG-1690 Basic information
- Product Name:
- GLPG-1690
- Synonyms:
-
- GLPG-1690
- 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
- CS-2644
- GLPG 1690;GLPG1690
- GLPG-1690; GLPG 1690; GLPG1690; ZIRITAXESTAT.
- ziritaxestat
- 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)-
- GLPG11690
- CAS:
- 1628260-79-6
- MF:
- C30H33FN8O2S
- MW:
- 588.7
- Product Categories:
-
- APIS
- API
- Mol File:
- 1628260-79-6.mol
GLPG-1690 Chemical Properties
- Density
- 1.42±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:70.84(Max Conc. mg/mL);120.32(Max Conc. mM)
Ethanol:4.0(Max Conc. mg/mL);6.79(Max Conc. mM) - form
- A crystalline solid
- pka
- 13.72±0.20(Predicted)
- color
- White to off-white
- InChIKey
- REQQVBGILUTQNN-UHFFFAOYSA-N
- SMILES
- S1C(C#N)=C(C2=CC=C(F)C=C2)N=C1N(C1N2C(=NC=1CC)C(C)=CC(N1CCN(CC(N3CC(O)C3)=O)CC1)=C2)C
GLPG-1690 Usage And Synthesis
Uses
GLPG1690 is a selective autotaxin inhibitor discovered by Galapagos, with potential application in idiopathic pulmonary disease (IPF). In a Phase 1 study in healthy human volunteers, GLPG1690 demonstrated favorable safety and tolerability, as well as a strong pharmacodynamic signal implying target engagement.
in vivo
Ziritaxestat (GLPG1690) inhibits ATX-induced LPA 18:2 production in mouse, rat, and healthy donor plasma in a concentration-dependent manner, with IC50 values of 418 nM, 542 nM, and 242 nM, respectively.Ziritaxestat (GLPG1690) displays improved pharmacokinetic properties, with a low plasma clearance and high bioavailability in mouse and rat. The good pharmacokinetic profile is further confirmed in dog, with Ziritaxestat (GLPG1690) showing low plasma clearance (0.12 L/h/kg) and a high bioavailability (63%)[1].
IC 50
Autotaxin: 131 nM (IC50); Autotaxin: 15 nM (Ki)
GLPG-1690Supplier
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