BAY-0069
Names
[ CAS No. ]:
420826-65-9
[ Name ]:
BAY-0069
Biological Activity
[Description]:
BAY-0069 is a potent and selective PPARγ inverse agonist with an IC50 value of 6.3 nM and 24 nM for human PPARγ and mouse PPARγ. BAY-0069 can be used to research cancer[1].
[Related Catalog]:
[Target]
hPPARγ:6.3 nM (IC50)
mouse PPARγ:24 nM (IC50)
[In Vitro]
BAY-0069 inhibits CYP2C8 with an IC50 of 4.3 μM[1]. BAY-0069 (0.1 nM-1 μM; 7 days) leads to antiproliferative effects in the PPARγ-amplified cell line UM-UC-9[1]. Cell Proliferation Assay[1] Cell 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 IC50 of 2.54 nM.
[In Vivo]
BAY-0069 (1 μM; 1 h) exhibits excellent microsomal stability with CLb,hmic of 0.47 L/h/kg in human liver microsomes and CLb,rhep of 3.9 L/h/kg in rat liver hepatocytes[1]. Pharmacokinetic Parameters of BAY-0069 in female NMRI nu/nu mice[1]. Route P.O. (100 mg/kg) I.P. S.C. AUC0-tlast (mg/L·h) 0.074 0.26 0.045 Cmax (nM) 35 59 4.4
Chemical & Physical Properties
[ Molecular Formula ]:
C22H16BrN3O4
[ Molecular Weight ]:
466.28