BI-2545

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BI-2545 是一种新型有效、选择性、口服 Autotaxin 抑制剂，对人和大鼠 ATX 的 IC50 值分别为 2.1 和 3.4 nM。

BI-2545 is a novel potent, selective, orally available Autotaxin inhibitor with IC50 of 2.1 and 3.4 nM for huamn and rat ATX, respectively; displays good potency in the LPA and rat whole blood assay (IC50=29 nM); shows substantial lowering of LPA in vivo, and excellent PK/Target Engagement relationship.

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

BI-2545 (10 mg/kg; p.o.) has high and sustained in vivo efficacy in reducing LPAs.BI-2545 (10 mg/kg; p.o.) has a half-life of t1/2=3.4 hours. Animal Model:Rat Dosage:10 mg/kg Administration:Oral administration Result:Reduces the sum of the plasma LPA species up to 90%.

BI2545 | BI 2545

Wnt/Notch/Hedgehog

Autotaxin

Autotaxin

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2162961-71-7

527.427

C23H19F6N5O3

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (474.01 mM)

O=C(N1C[C@]2([H])[C@H](CNC(C3=CC=C(NN=N4)C4=C3)=O)[C@]2([H])C1)OCC5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5

3,5-bis(trifluoromethyl)benzyl (1R,5S,6r)-6-((1H-benzo[d][1,2,3]triazole-5-carboxamido)methyl)-3-azabicyclo[3.1.0]hexane-3-carboxylate

(-20℃)

With Ice Pack

≥ 2 years