产品描述: | BPHA 是一种有效的具有口服活性的 MMP-2、MMP-9 和 MMP-14 抑制剂,IC50 分别为 12 nM、16 nM 和 17 nM。BPHA 不抑制 MMP-1、-3 和 -7 (IC50 分别为 974、>1000 和 795 nM)。BPHA 具有抗血管生成和抗肿瘤作用。 |
靶点: |
MMP-2:12 nM (IC50);MMP-9:16 nM (IC50);MMP |
体外研究: |
BPHA does not inhibit typical serine proteinases (neutrophil elastase, plasmin, trypsin, and chymotrypsin), cysteine proteinases (cathepsins B and L), aspartic proteinase (HIV-1 protease), or metalloproteinase (aminopeptidase M). |
体内研究: |
Daily oral administration of 200 mg/kg BPHA in mice results in potent inhibition of tumor-induced angiogenesis, primary tumor growth, and liver metastasis. The growth inhibition activity of BPHA is 48% and 45% in a B16-BL6 melanoma and F2 hemangio-endothelioma model, respectively. |
参考文献: |
1. R Maekawa, et al. Correlation of antiangiogenic and antitumor efficacy of N-biphenyl sulfonyl-phenylalanine hydroxiamic acid (BPHA), an orally-active, selective matrix metalloproteinase inhibitor. Cancer Res. 1999 Mar 15;59(6):1231-5. |
保存条件: |
-20℃,密闭,干燥 |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.522 ml |
12.612 ml |
25.223 ml |
5 mM |
0.504 ml |
2.522 ml |
5.045 ml |
10 mM |
0.252 ml |
1.261 ml |
2.522 ml |
50 mM |
0.05 ml |
0.252 ml |
0.504 ml |
|
注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |