BAY-0069

• 常用名: BAY-0069
• 英文名: BAY-0069
• CAS号: 420826-65-9
• 分子量: 466.28
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₂H₁₆BrN₃O₄
• 熔点: N/A
• 闪点: N/A

BAY-0069用途

BAY-0069是一种有效的选择性PPARγ反向激动剂,对人PPARγ和小鼠PPARγ的IC50值分别为6.3nM和24nM。BAY-0069可用于研究癌症[1]。

BAY-0069名称

• 英文名: BAY-0069

BAY-0069生物活性

• 描述: BAY-0069是一种有效的选择性PPARγ反向激动剂,对人PPARγ和小鼠PPARγ的IC50值分别为6.3nM和24nM。BAY-0069可用于研究癌症[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 细胞周期/DNA损伤 >> PPAR
• 靶点实验:

  hPPARγ:6.3 nM (IC50)

  mouse PPARγ:24 nM (IC50)

• 体外研究: BAY-0069以4.3μM的IC50抑制CYP2C8[1]。BAY-0069(0.1 nM-1μM；7天)导致PPARγ扩增细胞系UM-UC-9[1]的抗增殖作用。细胞增殖测定[1]细胞系：PPARγ-扩增的细胞系UM-UC-9浓度：0.0001、0.001、0.01、0.01和1μM培养时间：7天结果：抑制PPARγ扩增的细胞株UM-UC-7,IC50为2.54nM。
• 体内研究: BAY-0069(1μM；1小时)表现出优异的微粒体稳定性,人肝微粒体中CLb,hmic为0.47 L/h/kg,大鼠肝细胞中CLb的rhep为3.9 L/h/kg[1]。BAY-0069在雌性NMRI nu/nu小鼠中的药代动力学参数[1]。路线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

BAY-0069物理化学性质

• 分子式: C₂₂H₁₆BrN₃O₄
• 分子量: 466.28
• InChIKey: BJSIVXYQIGFUCG-UHFFFAOYSA-N
• SMILES: CCc1ccc(-c2nc3cc(NC(=O)c4cc([N+](=O)[O-])ccc4Br)ccc3o2)cc1

BAY-0069靶点实验

查看更多实验

实验名称：Inverse agonist activity at GAL4-tagged mouse PPARgamma LBD expressed in CHO cells me... 来源：ChEMBL 靶标：Peroxisome proliferator-activated receptor gamma External Id：CHEMBL5113082

实验名称：Inverse agonist activity at GAL4-tagged human PPARgamma LBD expressed in CHO cells me... 来源：ChEMBL 靶标：Peroxisome proliferator-activated receptor gamma External Id：CHEMBL5113084

实验名称：Efflux ratio of apparent permeability across basolateral to apical side to apparent p... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5113078

实验名称：Thermodynamic solubility of the compound in PBS at pH 6.5 measured after 24 hrs by HP... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5113079

实验名称：Covalent binding affinity to recombinant human PPARgamma at 5 uM measured by mass spe... 来源：ChEMBL 靶标：Peroxisome proliferator-activated receptor gamma External Id：CHEMBL5113080

实验名称：Stability of compound in 500 uM cysteine at pH 7.4 assessed as compound recovered at ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5113074

实验名称：Stability of compound in 500 uM cysteine at pH 7.4 assessed as compound recovered at ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5113075

实验名称：Apparent permeability of the compound across apical side to basolateral side in human... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5113077

实验名称：Stability of compound in 500 uM glutathione at pH 7.4 assessed as compound recovered ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5113070

实验名称：Stability of compound in 500 uM glutathione at pH 7.4 assessed as compound recovered ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5113071

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