| CAS |
No.150045-18-4 |
| 英文名称 |
MRT-83 |
| 分子式 |
C31H30N4O5 |
| 分子量 |
538.59 |
| 溶解性 |
Soluble in DMSO |
| 纯度 |
≥98% |
| 外观(性状) |
Light yellow to yellow Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| SMILES |
COC1=C(OC)C(OC)=CC(C(NC(NC2=CC(NC(C3=CC=C(C4=CC=CC=C4)C=C3)=O)=C(C)C=C2)=N)=O)=C1 |
| InChIKey |
BKTMNLKJWHVZRN-UHFFFAOYSA-N |
| InChI |
InChI=1S/C31H30N4O5/c1-19-10-15-24(33-31(32)35-30(37)23-16-26(38-2)28(40-4)27(17-23)39-3)18-25(19)34-29(36)22-13-11-21(12-14-22)20-8-6-5-7-9-20/h5-18H,1-4H3,(H,34,36)(H3,32,33,35,37) |
| PubChem CID |
136210511 |
| 靶点 |
Smo |
| 通路 |
Hedgehog;Stem Cells |
| 背景说明 |
MRT-83是 Smoothened (Smo) 受体的有效拮抗剂。 |
| 生物活性 |
MRT-83 is a potent antagonist of Smo， with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.[1] |
| In Vitro |
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[1]. |
| In Vivo |
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[1]. |
| 动物实验 |
Mice[1]Four groups of six animals received 5 μL of 45% 2-hydroxypropyl-β-cyclodextrin PBS solution containing 0.9 μg of ShhN alone or in the presence of MRT-83 (200 ng) or MRT-36 (110 ng). A control group receive 5 μL of 45% 2-hydroxypropyl-β-cyclodextrin solution alone. All groups are analyzed 48 h after the injection[1] |
| 数据来源文献 |
[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. |
| 规格 |
1mg 5mg 10mg 25mg 50mg 100mg |
| 单位 |
瓶 |
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