MRT-10

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MRT-10 

MRT-10 是一种七跨膜平滑受体 (Smo) 拮抗剂,在各种 Hedgehog (Hh) 测定中,IC50 为 0.65 μM。MRT-10 在 Bodipycyclopamine 结合位点水平与 Smo 受体结合。MRT-10可用于癌症研究。

MRT-10

MRT-10 Chemical Structure

CAS No. : 330829-30-6

规格 价格 是否有货 数量
5 mg ¥1800 In-stock
10 mg ¥2800 In-stock
25 mg ¥5900 In-stock
50 mg ¥9500 In-stock
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200 mg   询价  

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MRT-10 相关产品

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生物活性

MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer[1][2].

体外研究
(In Vitro)

MRT-10 inhibits the Smo-induced IP accumulation in a dosedependent manner (IC50=2.5 μM) in HEK293 cells[1].
MRT-10 (10-9-10-5 M; 2 h) blocks Bodipy-cyclopamine (5 nM; 2 h) binding to cells expressing mouse Smo in a dosedependent manner with an IC50=0.5 μM[1].
MRT-10 (10-9-10-5 M; 40 h) inhibits ShhN signaling in Shh-light2 cells in a dose-dependent manner with an IC50=0.64 μM[1].
MRT-10 (10-9-10-5 M; 6 days) inhibits the SAG-induced (0.1 μM) alkaline phosphatase (AP) activity with an IC50=0.90 μM ) in C3H10T1/2 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

465.52

Formula

C24H23N3O5S

CAS 号

330829-30-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (214.81 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1481 mL 10.7407 mL 21.4814 mL
5 mM 0.4296 mL 2.1481 mL 4.2963 mL
10 mM 0.2148 mL 1.0741 mL 2.1481 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.37 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Manetti F, et al. Virtual screening-based discovery and mechanistic characterization of the acylthiourea MRT-10 family as smoothened antagonists. Mol Pharmacol. 2010 Oct;78(4):658-65.

    [2]. Solinas A, et al. Acylthiourea, acylurea, and acylguanidine derivatives with potent hedgehog inhibiting activity. J Med Chem. 2012 Feb 23;55(4):1559-71.

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