BAY-0069

Research use only, not for human use.

BAY-0069 is a potent and selective PPARγ transactivator, inhibiting human PPARγ and murine PPARγ with IC50 values of 6.3 nM and 24 nM, respectively. BAY-0069 can be used in cancer research.

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.

BAY-0069 inhibits CYP2C8 with an IC50 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.Cell Proliferation Assay 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.

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.Pharmacokinetic Parameters of BAY-0069 in female NMRI nu/nu mice.

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Metabolic Enzyme/Protease

PPAR

PPAR

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420826-65-9

466.28

C22H16BrN3O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (214.46 mM; Ultrasonic (<60°C)

N(C(=O)C1=CC(N(=O)=O)=CC=C1Br)C=2C=C3C(OC(=N3)C4=CC=C(CC)C=C4)=CC2

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(-20℃)

With Ice Pack

≥ 2 years