Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptorNur77/NR4A1agonist with anEC₅₀of 0.278 nM.

EC50: 0.278 nM (Nur77)^[1]

Cytosporone B targets the ligand binding domain of Nur77, which selectively stimulates the transactivational activity of Nur77. Cytosporone B induces luciferase activity in cells that are cotransfected with GAL4- Nur77 or GAL4-LBD. The EC₅₀of cytosporone B for Nur77 is 0.278 nM. Cytosporone B displays robust pro-apoptotic activity in gastric cancer cells BGC-823. 63.5% of the cells are apoptotic when treated with cytosporone B for 48 h. Cytosporone B shows selective effect on cancerous cells. Cytosporone B inhibits proliferation of human gastric cancer BGC-823 cells and human colon cancer SW620 cells by 470%, but it has a modest effect on human lung cancer H1299 cells and human hepatoma HepG2 cells^[1].

In the hepatocytes of wild-type mice, the transcriptional activity of the reporter is induced five-fold with cytosporone B treatment. In wild-type mice, cytosporone B treatment significantly increases glucose levels from 3.2 to 11.4 mM within the first 30 min, and thereafter blood glucose gradually decreased before reaching the initial level after 300 min^[1].

322.40

Solid

C₁₈H₂₆O₅

321661-62-5

• Phenols
• Polyphenols

• Others

fungus Eupenicillium sp. HJ002

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 100 mg/mL(310.17 mM)

Ethanol : ≥ 50 mg/mL(155.09 mM)

*"≥" means soluble, but saturation unknown.

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: ≥ 2.5 mg/mL (7.75 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.75 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (7.75 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.75 mM，饱和度未知) 的澄清溶液。

  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 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