store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 20 mg/mL (47.12 mM), sonification is recommended.
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
Dihydromunduletone 674786-20-0 Endocrinology/Hormones GPCR/G Protein GPR DHM Inhibitor inhibitor inhibit