BAY-0069

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BAY-0069

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

420826-65-9

BAY-0069 是一种有效且具有选择性的PPARγ反向激活剂，对人 PPARγ 和鼠 PPARγ 的IC₅₀分别为 6.3 nM 和 24 nM。BAY-0069 可用于癌症的研究。

生物活性

BAY-0069 is a potent and selectivePPARγinverse agonist with anIC₅₀value of 6.3 nM and 24 nM for humanPPARγand mousePPARγ. BAY-0069 can be used to researchcancer^[1].

IC₅₀& Target^[1]

hPPARγ

6.3 nM (IC₅₀)

mouse PPARγ

24 nM (IC₅₀)

体外研究
(In Vitro)

BAY-0069 inhibits CYP2C8 with an IC₅₀of 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 IC₅₀of 2.54 nM.

体内研究
(In Vivo)

BAY-0069 (1 μM; 1 h) exhibits excellent microsomal stability with CL_b,hmicof 0.47 L/h/kg in human liver microsomes and CL_b,rhepof 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.
AUC_0-tlast(mg/L·h)	0.074	0.26	0.045
C_max(nM)	35	59	4.4

分子量

466.28

Formula

C₂₂H₁₆BrN₃O₄

CAS 号

420826-65-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.