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: 20.9 μM (GPR56)^[1]; GPR114^[1]

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].

424.49

Solid

C₂₅H₂₈O₆

674786-20-0

Room temperature in continental US; may vary elsewhere.

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

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。

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。