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Dihydromunduletone

Dihydromunduletone

产品编号 T11044   CAS 674786-20-0
别名: DHM

Dihydromunduletone (DHM) 是一种粘附 G 蛋白偶联受体 (aGPCR)拮抗剂,可做一种化学探针,对具有相似拴系激动剂的 GPR56 和 GPR114/ADGRG5 有抑制作用。

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Dihydromunduletone Chemical Structure
Dihydromunduletone, CAS 674786-20-0
规格 价格/CNY 货期 数量
5 mg ¥ 4,980 现货
10 mg ¥ 9,380 5日内发货
1 mL * 10 mM (in DMSO) ¥ 5,370 现货
产品目录号及名称: Dihydromunduletone (T11044)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Dihydromunduletone (DHM) is an adhesion G protein-coupled receptor (aGPCR) antagonist that acts as a chemical probe for the inhibition of GPR56 and GPR114/ADGRG5, which have similar tethered agonists.
靶点活性 GPR56:20.9 μM
体外活性 Assays are initiated by the addition of [35S]GTPγS, and the rates of aGPCR-stimulated G protein activation (Gα binding to [35S]GTPγS) are measured with or without the influence of added compounds. Dihydromunduletone (DHM) inhibits the kinetics of GPR56 7TM-stimulated G13 GTPγS binding to varying degrees. Among the inhibitory compounds tested, Dihydromunduletone is the most effective, reducing the rate at which GPR56 7TM activates G13 by over 75% (from 0.18 to 0.04 minute−1)[1].At a concentration of Dihydromunduletone (DHM) that maximally inhibits GPR56 (50 μM), the rate of GPR114 7TM-stimulated Gs activity is also dramatically inhibited. However, when Dihydromunduletone (50 μM) is applied to GPR110 7TM, it fails to inhibit GPR110 stimulation of Gq GTPγS binding[1].
Cells transfected with GPR56 A386M 7TM are incubated with increasing concentrations of Dihydromunduletone. After adding the P7 peptide agonist, SRE-luciferase activity is measured. Dihydromunduletone inhibits P7 peptide-induced luciferase activity in a concentration-dependent manner. Additionally, cells treated with a fixed concentration of 3 µM Dihydromunduletone and then stimulated with an increasing concentration of P7 peptide agonist show that Dihydromunduletone treatment blunts P7 peptide activation at each concentration. In conclusion, Dihydromunduletone antagonizes synthetic-peptide agonist and tethered-peptide agonist-mediated aGPCR activation in isolated membranes and HEK293T cell-based assays, but it does not inhibit basal receptor signaling[1].
别名 DHM
分子量 424.49
分子式 C25H28O6
CAS No. 674786-20-0

存储

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 20 mg/mL (47.12 mM), sonification is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3558 mL 11.7788 mL 23.5577 mL 58.8942 mL
5 mM 0.4712 mL 2.3558 mL 4.7115 mL 11.7788 mL
10 mM 0.2356 mL 1.1779 mL 2.3558 mL 5.8894 mL
20 mM 0.1178 mL 0.5889 mL 1.1779 mL 2.9447 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Hannah M. Stoveken, et al. Dihydromunduletone Is a Small-Molecule Selective Adhesion G Protein–Coupled Receptor Antagonist. Mol Pharmacol. 2016 Sep; 90(3): 214–224.
(2-{[2-(2-fluorophenoxy)ethyl]sulfanyl}-1H-benzimidazol-1-yl)acetic acid Monomethyl fumarate Kuwanon H GPCR agonist-2 AS1269574 YUM70 PU-H54 MBX-2982

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Dihydromunduletone 674786-20-0 Endocrinology/Hormones GPCR/G Protein GPR DHM Inhibitor inhibitor inhibit

 

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