| Bioactivity | 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]. | ||||||||||||
| Target | C50: 2.2 nM (human ATX), 3.4 nM (rat ATX) | ||||||||||||
| Invitro | BI-2545 displays good potency in the LPA and rat whole blood assay with IC50s of 29 nM and 96 nM, respectively[1]. | ||||||||||||
| In Vivo | 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: | ||||||||||||
| Name | BI-2545 | ||||||||||||
| CAS | 2162961-71-7 | ||||||||||||
| Formula | C23H19F6N5O3 | ||||||||||||
| Molar Mass | 527.42 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
BI-2545
CAS: 2162961-71-7 F: C23H19F6N5O3 W: 527.42
BI-2545 is a potent autotaxin (ATX) inhibitor that significantly reduces LPA, with IC50s of 2.2 nM and 3.4 nM for human
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