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MRT-83 Sale

目录号 : GC33114

MRT-83是有效的Smo拮抗剂,其IC50值在纳摩尔级别。

MRT-83 Chemical Structure

Cas No.:1263131-92-5

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5mg
¥1,080.00
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10mg
¥1,710.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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实验参考方法

Animal experiment:

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]

References:

[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.

产品描述

MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range.

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].

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].

[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.

Chemical Properties

Cas No. 1263131-92-5 SDF
Canonical 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
分子式 C31H30N4O5 分子量 538.59
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.8567 mL 9.2835 mL 18.567 mL
5 mM 0.3713 mL 1.8567 mL 3.7134 mL
10 mM 0.1857 mL 0.9283 mL 1.8567 mL
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