MRT-83

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MRT-83 是一种有效的 Smo 拮抗剂。

MRT-83 is a potent Smo antagonist.(In Vitro):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 assays.(In Vivo): MRT-83 can't up-regulation of Ptc transcription in the SVZ of these animals in agreement with 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 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 assays.

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.

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Wnt/Notch/Hedgehog

Smoothened (Smo)

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1263131-92-5

538.604

C31H30N4O5

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (464.17 mM)

COc1cc(cc(OC)c1OC)C(=O)NC(=N)Nc1ccc(C)c(NC(=O)c2ccc(cc2)-c2ccccc2)c1

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(-20℃)

With Ice Pack

≥ 2 years