| 产品描述： | MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling |
| 靶点： |
Smo |
| 体外研究： |
MRT-83 displays full antagonist properties with an IC50 (~3 nM) for inhibiting ShhN (3 nM)-induced proliferation of rat GCPs. MRT-83 also blocks SAG (0.01 μM)-induced proliferation of GCPs (IC50 ~6 nM). MRT-83 blocks BC binding to HEK-hSmo cells in a dose-dependent manner with an IC50 of 4.6 nM. MRT-83 abrogates BC binding to cells expressing mouse Smo with an IC50 of 14 nM, which is in good correlation with its IC50 in the Shh-light2 and alkaline phosphatase assays1. |
| 体内研究： |
Animals treated with ShhN in the presence of MRT-83 are as healthy as those of the other groups but up-regulation of Ptc transcription in the SVZ of these animals is no longer observed in agreement with a complete inhibition of ShhN-mediated effects (8.7±2.4 Ptc+ cells/section, n=9) and is not different from vehicle-mediated effects. MRT-83 but not MRT-36 antagonizes the up-regulation of Ptc transcription induced by ShhN in vivo in the SVZ of the LV. |
| 参考文献： |
1. Roudaut H, et al. Identification and mechanism of action of the acylguanidine MRT-83, a novel potent Smoothened antagonist. Mol Pharmacol. 2011 Mar;79(3):453-60. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 备注： |
MRT-83 是有效的 Smo 拮抗剂，其 IC50 值在纳摩尔级别。MRT-83 也抑制 Hedgehog (Hh) 信号通路。 |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.857 ml |
9.283 ml |
18.567 ml |
| 5 mM |
0.371 ml |
1.857 ml |
3.713 ml |
| 10 mM |
0.186 ml |
0.928 ml |
1.857 ml |
| 50 mM |
0.037 ml |
0.186 ml |
0.371 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