BI-2545 是一种高效的 autotaxin (ATX) 抑制剂，可显著降低 LPA 的水平，对人和大鼠的 ATX 作用 IC50 值分别为 2.2 nM 和3.4 nM。
货号:ajcx29164
CAS:2162961-71-7
分子式:C23H19F6N5O3
分子量：527.42
溶解度:DMSO: 250 mg/mL (474.01 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BI-2545 is a potent autotaxin (ATX) inhibitor that significantly reduces LPA, with IC50s of 2.2 nM and 3.4 nM for human ATX and rat ATX, respectively[1].

BI-2545 displays good potency in the LPA and rat whole blood assay with IC50s of 29 nM and 96 nM, respectively[1].

BI-2545 (10 mg/kg; p.o.) has high and sustained in vivo efficacy in reducing LPAs[1].BI-2545 (10 mg/kg; p.o.) has a half-life of t1/2=3.4 hours[1]. Animal Model: Rat[1]

[1]. Kuttruff, C. A., et al. Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo. ACS Medicinal Chemistry Letters, 8(12), 1252-1257.