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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
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
GLPG1690 (GLPG1690) 是一流的 autotaxin (ATX) 抑制剂，IC50 为 131 nM，Ki 为 15 nM。
Cas No.1628260-79-6
别名GLPG1690
Canonical SMILESN#CC1=C(C2=CC=C(F)C=C2)N=C(N(C3=C(CC)N=C4C(C)=CC(N5CCN(CC(N6CC(O)C6)=O)CC5)=CN43)C)S1
分子式C30H33FN8O2S
分子量588.7
溶解度DMSO : 41.67 mg/mL (70.78 mM);Water :< 0.1 mg/mL (insoluble)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

References:
[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.