1. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. PPAR
  3. BAY-0069

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.

For research use only. We do not sell to patients.

BAY-0069 Chemical Structure

BAY-0069 Chemical Structure

CAS No. : 420826-65-9

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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].

IC50 & Target[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

466.28

Formula

C22H16BrN3O4

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC1=CC=C(OC(C2=CC=C(CC)C=C2)=N3)C3=C1)C4=CC([N+]([O-])=O)=CC=C4Br

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (214.46 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1446 mL 10.7232 mL 21.4463 mL
5 mM 0.4289 mL 2.1446 mL 4.2893 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1446 mL 10.7232 mL 21.4463 mL 53.6159 mL
5 mM 0.4289 mL 2.1446 mL 4.2893 mL 10.7232 mL
10 mM 0.2145 mL 1.0723 mL 2.1446 mL 5.3616 mL
15 mM 0.1430 mL 0.7149 mL 1.4298 mL 3.5744 mL
20 mM 0.1072 mL 0.5362 mL 1.0723 mL 2.6808 mL
25 mM 0.0858 mL 0.4289 mL 0.8579 mL 2.1446 mL
30 mM 0.0715 mL 0.3574 mL 0.7149 mL 1.7872 mL
40 mM 0.0536 mL 0.2681 mL 0.5362 mL 1.3404 mL
50 mM 0.0429 mL 0.2145 mL 0.4289 mL 1.0723 mL
60 mM 0.0357 mL 0.1787 mL 0.3574 mL 0.8936 mL
80 mM 0.0268 mL 0.1340 mL 0.2681 mL 0.6702 mL
100 mM 0.0214 mL 0.1072 mL 0.2145 mL 0.5362 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
BAY-0069
Cat. No.:
HY-148351
Quantity:
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