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Ziritaxestat(GLPG-1690)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ziritaxestat(GLPG-1690)图片
CAS NO:1628260-79-6
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 588.71
Formula C30H33FN8O2S
CAS No. 1628260-79-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 80 mg/mL
Water: N/A
Ethanol: N/A
Solubility (In vivo) CCC(N=C1N2C=C(C=C1C)N3CCN(CC3)CC(N4CC(C4)O)=O)=C2N(C)C5=NC(C6=CC=C(C=C6)F)=C(S5)C#N
Synonyms GLPG 1690; Ziritaxestat; GLPG1690; GLPG-1690
实验参考方法
In Vitro

In vitro activity: GLPG1690 is a potent and the first selective autotaxin (ATX) inhibitor with IC50 of 131 nM and Ki of 15 nM. GLPG1690 has the potential applications in the treatment of idiopathic pulmonary disease (IPF). GLPG1690 showed 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 GLPG1690 showing low plasma clearance (0.12 L/h/kg) and a high bioavailability (63%). In a Phase 1 study, GLPG1690 demonstrated favorable safety and tolerability profile, as well as a strong pharmacodynamic signal implying target engagement.


Kinase Assay: GLPG1690 is a potent and the first selective autotaxin (ATX) inhibitor with IC50 of 131 nM and Ki of 15 nM. GLPG1690 shows no CYP3A4 TDI and decreases hERG inhibitory activity with IC50 of 15 μM in manual patch clamp assay


Cell Assay: Ziritaxestat (formerly GLPG1690) is a potent and a first-in-class selective autotaxin (ATX) inhibitor (IC50 = 131 nM and Ki of 15 nM) with the potential to be used in the treatment of idiopathic pulmonary disease (IPF). As of Feb 2021, the phase 3 trial has failed. GLPG1690 showed 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 GLPG1690 showing low plasma clearance (0.12 L/h/kg) and a high bioavailability (63%). In a Phase 1 study, GLPG1690 demonstrated favorable safety and tolerability profile, as well as a strong pharmacodynamic signal implying target engagement.


In VivoGLPG1690 inhibits ATX-induced LPA 18:2 production in mouse, rat, and healthy donor plasma in a concentration-dependent manner, with IC50values of 418 nM, 542 nM, and 242 nM, respectively. 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 GLPG1690 showing low plasma clearance (0.12 L/h/kg) and a high bioavailability (63%)。
Animal modelNA
Formulation & DosageNA
References J Med Chem. 2017 May 11;60(9):3580-3590.