您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Dihydromunduletone
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Dihydromunduletone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dihydromunduletone图片
CAS NO:674786-20-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
DHM
产品介绍
Dihydromunduletone (DHM) 是类胡萝卜素衍生物,是一种选择性,有效的粘附 G 蛋白偶联受体 (aGPCR) (GPR56 and GPR114/ADGRG5) 拮抗剂,对GPR56IC50值为 20.9 μM,但不抑制 GPR110 或 A 类 GPCR。
生物活性

Dihydromunduletone (DHM) is a rotenoid derivative and a selective, potentadhesion G protein-coupled receptor (aGPCR)(GPR56 and GPR114/ADGRG5) antagonist with anIC50of 20.9 μM forGPR56, but not inhibit GPR110 or class A GPCRs[1].

IC50& Target

IC50: 20.9 μM (GPR56)[1]; GPR114[1]

体外研究
(In Vitro)

Assays are initiated by the addition of [35S]GTPγS, and the rates of aGPCR-stimulated G protein activation ([35S]GTPγS binding to Gα) 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. Dihydromunduletone is the best inhibitory compound and reduced the rate at which GPR56 7TM activated G13 >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 inhibited dramatically. When Dihydromunduletone (50 μM) is applied to the 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. P7 peptide agonist is added, and SRE-luciferase activity is measured. Dihydromunduletone inhibits the P7 peptide-induced luciferase activity in a concentration-dependent manner. Cells are also treated with a fixed concentration of 3 μM Dihydromunduletone and then stimulated with an increasing concentration of P7 peptide agonist. 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].

Clinical Trial
分子量

424.49

性状

Solid

Formula

C25H28O6

CAS 号

674786-20-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL(588.94 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3558 mL11.7788 mL23.5577 mL
5 mM0.4712 mL2.3558 mL4.7115 mL
10 mM0.2356 mL1.1779 mL2.3558 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.90 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 20.8 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本网站选购。