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BAY-0069 is a potent and selective PPARγ inverse agonist with an IC 50 value of 6.3 nM and 24 nM for human PPARγ and mouse PPARγ . BAY-0069 can be used to research cancer
In Vitro
BAY-0069 inhibits CYP2C8 with an IC 50 of 4.3 μM. BAY-0069 (0.1 nM-1 μM; 7 days) leads to antiproliferative effects in the PPARγ-amplified cell line UM-UC-9. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: PPARγ-amplified cell line UM-UC-9 Concentration: 0.0001, 0.001, 0.01, 0.01 and 1 μM Incubation Time: 7 days Result: Inhibited PPARγ-amplified cell line UM-UC-9 with an IC 50 of 2.54 nM.
In Vivo
BAY-0069 (1 μM; 1 h) exhibits excellent microsomal stability with CL b,hmic of 0.47 L/h/kg in human liver microsomes and CL b,rhep of 3.9 L/h/kg in rat liver hepatocytes . Pharmacokinetic Parameters of BAY-0069 in female NMRI nu/nu mice . Route P.O. (100 mg/kg) I.P. S.C. AUC 0-tlast (mg/L·h) 0.074 0.26 0.045 C max (nM) 35 59 4.4 MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:hPPARγ 6.3 nM (IC 50 ) mouse PPARγ 24 nM (IC 50 )