Ziritaxestat (GLPG1690) 是创新的 autotaxin (ATX) 抑制剂，IC₅₀ 和 K_i 值分别为 131 nM 和 15 nM。

Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with an IC 50 of 131 nM and a K i of 15 nM.

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Autotaxin 131 nM (IC50) Autotaxin 15 nM (K

Ziritaxestat (GLPG1690) shows no CYP3A4 TDI and decreases hERG inhibitory activity with IC50 of 15 μM in manual patch clamp assay. has not independently confirmed the accuracy of these methods. They are for reference only.

Ziritaxestat (GLPG1690) inhibits ATX-induced LPA 18:2 production in mouse, rat, and healthy donor plasma in a concentration-dependent manner, with IC 50 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%). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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 Cli

In Vitro: DMSO : 41.67 mg/mL (70.78 mM; Need ultrasonic)配制储备液