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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Autotaxin-GLPG1690
GLPG1690

Chemical Structure : GLPG1690

CAS No.: 1628260-79-6

GLPG1690 (Ziritaxestat, GLPG 1690)

货号: PC-60402Not For Human Use, Lab Use Only.

GLPG1690 (Ziritaxestat, GLPG 1690) is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM.

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10 mg ¥880 In stock
25 mg ¥1380 In stock
50 mg ¥2180 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GLPG1690 (Ziritaxestat, GLPG 1690) is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM.
GLPG1690 (Ziritaxestat) inhibits ATX-induced LPA 18:2 production in mouse, rat, and healthy donor plasma with IC50 of 418 nM, 542 nM, and 242 nM, respectively.
GLPG1690 (Ziritaxestat shows no CYP3A4 TDI and decreased hERG inhibitory activity (IC50=15 uM), and good pharmacokinetic profile for treatment idiopathic pulmonary fibrosis.
GLPG1690 also is an inhibitor of the ectonucleotide pyrophosphatase/ phosphodiesterase family (ENPP2).

物理化学性质&存储条件

分子量 588.71
分子式 C30H33FN8O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Desroy N, et al. J Med Chem. 2017 May 11;60(9):3580-3590.

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