| 产品描述： | S-methyl-KE-298 is an active metabolite of KE-298. KE-298 inhibits matrix metalloproteinase (MMP-1) production from rheumatoid arthritis (RA) synovial cells. |
| 靶点： |
MMP;Drug Metabolite |
| 体外研究： |
S-methyl-KE-298 is a methyl conjugate of deacetyl-KE-298 is plasma. In vitro protein binding of KE-298 and its plasma metabolites, deacetyl-KE-298 (M-1) and S-methyl-KE-298 (M-2), is high in rat (>97%), dog (>89%) and human plasma (>99%), respectively. KE-298 blocks this IL-1β-induced pro-MMP-2 activation and MT1-MMP expression, but does not affect IL-1β-induced tissue inhibitor of metalloproteinase-2 (TIMP-2) secretion from rheumatoid synovial cells. KE-298 inhibits MMP-1 production from rheumatoid arthritis (RA) synovial cells by affecting a transcription factor, AP-1. KE-298 inhibits the basal levels of MT1-MMP expression of unstimulated rheumatoid synovial cells |
| 参考文献： |
1. Yoshida H, et al. Identification of metabolites of KE-298, a new antirheumatic drug, and its physiological properties in rats. Biol Pharm Bull. 1996 Mar;19(3):424-9. 2. Endo H, et al. Stereoselectivity and species difference in plasma protein binding of KE-298 and its metabolites. Biol Pharm Bull. 2001 Jul;24(7):800-5. 3. Honda S, et al. Expression of membrane-type 1 matrix metalloproteinase in rheumatoid synovial cells. Clin Exp Immunol. 2001 Oct;126(1):131-6. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.963 ml |
19.815 ml |
39.631 ml |
| 5 mM |
0.793 ml |
3.963 ml |
7.926 ml |
| 10 mM |
0.396 ml |
1.982 ml |
3.963 ml |
| 50 mM |
0.079 ml |
0.396 ml |
0.793 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京