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GLPG1690
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。
GLPG1690图片
CAS NO:1628260-79-6
规格:98%
分子量:588.7
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

产品介绍
GLPG1690 is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and Ki of 15 nM.
CAS:1628260-79-6
分子式:C30H33FN8O2S
分子量:588.7
纯度:98%
存储:Store at -20°C

Background:

GLPG1690 is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and Ki of 15 nM.


GLPG1690 shows no CYP3A4 TDI and decreases hERG inhibitory activity with IC50 of 15 uM in manual patch clamp assay[1].


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. 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%)[1].


参考文献:
[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 Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis. J Med Chem. 2017 May 11;60(9):3580-3590.