產(chǎn)品描述: | IWP L6 (Porcn Inhibitor III) is a Porcn inhibitor with an EC50 of 0.5 nM. |
靶點: |
EC50 Value: 0.5 nM;Porcupine |
體外研究: |
IWP-L6 (Porcn Inhibitor III) effectively suppressed the phosphorylation of dishevelled 2 (Dvl2) in HEK293 cells, a biochemical event associated with many Wnt-dependent cellular responses. IWP-L6 inhibits Wnt mediated branching morphogenesis in cultured embryonic kidneys . |
體內(nèi)研究: |
IWP-L6 (Porcn Inhibitor III) is stable in human plasma over 24 h, it was rapidly metabolized in rat plasma (t1/2 = 190 min), murine plasma (t1/2 = 2 min), and the murine liver S9 fractions (t1/2 = 26 min). The major metabolites are the amide cleavage products. Similar species-dependent metabolitic profiles due to the involvement of carboxylesterase (CES) have been reported with other drug candidates. Despite its modest metabolic stability in mouse-derived plasma, IWP-L6 was highly active in zebrafish. IWP-L6 exhibited more potent activity |
參考文獻: |
1. Wang, X., et al., The development of highly potent inhibitors for porcupine. J Med Chem, 2013. 56(6): p. 2700-4. |
溶解性: |
Soluble in DMSO |
保存條件: |
-20°C |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.116 ml |
10.58 ml |
21.16 ml |
5 mM |
0.423 ml |
2.116 ml |
4.232 ml |
10 mM |
0.212 ml |
1.058 ml |
2.116 ml |
50 mM |
0.042 ml |
0.212 ml |
0.423 ml |
|
注意: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。 |