Corticosterone (17-Deoxycortisol) 是一种具有口服活性的，由肾上腺皮质产生的糖皮质激素，在调节边缘系统 (包括海马体、前额叶皮层和杏仁核) 的神经元功能方面起着重要作用。皮质酮可通过SGK诱导的GDI磷酸化增加Rab介导的AMPAR膜运输。Corticosterone 还能干扰树突状细胞的成熟，具有较好的免疫抑制活性。
| 生物活性 | Corticosterone (17-Deoxycortisol) is an orally active and adrenal cortex-produced glucocorticoid, which plays an important role in regulating neuronal functions of the limbic system (including hippocampus, prefrontal cortex, and amygdala). Corticosterone increases theRab-mediatedAMPARmembrane traffic viaSGK-induced phosphorylation ofGDI. Corticosterone also interferes with the maturation of dendritic cells and shows a good immunosuppressive effect[1][2][3][4]. |
| IC50& Target | Human Endogenous Metabolite |
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体外研究
(In Vitro) | Corticosterone (100 nM; 30 min) via SGK phosphorylation of GDI at Ser-213, increases the formation of GDI-Rab4 complex, facilitating the functional cycle of Rab4 and Rab4-mediated recycling of AMPARs to the synaptic membrane[1].
Corticosterone (CORT) (1 μM; 48 h) shows good immunosuppressive properties (functionally compromises maturation of BMDC), which impairs LPS-induced up-regulation of maturation-associated markers (MHC class II, B7.2, B7.1 and CD40)[2].
Cell Viability Assay[1] | Cell Line: | HEK293 cells | | Concentration: | 100 nM | | Incubation Time: | 30 min | | Result: | Caused a significant enhancement of mEPSC amplitude (mEPSC represents the postsynaptic response to release of individual vesicles of glutamate).
Increased the transmission of glutamatergic, and increased synaptic AMPAR currents via a Rab4-dependent mechanism.
Profoundly increased surface GluR1 cluster density, cluster size and cluster fluorescence intensity.
Significantly increased the amount of Rab4 that binded to WT-GDI, S45A-GDI, or S121A-GDI but not S213A-GDI.
Induced the phosphorylation of GST-WTGDI, GST-S45AGDI, and GST-S121AGDI, but not GST-S213AGDI, and this effect was blocked in cells transfected with SGK1 small interfering RNA.
Increased AMPAR surface expression via a mechanism dependent on GDI phosphorylation. |
Cell Viability Assay[2] | Cell Line: | BMDC cells | | Concentration: | 1 μM | | Incubation Time: | 48 h | | Result: | Completely blocked the expression of MHC class II and B7.2 that induced by LPS, and maximally impaired BMDC cells maturation at 12 h.
Reduced B7.1 by 50%, and slightly down-regulated CD40. |
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体内研究
(In Vivo) | Corticosterone results in a marked reduction in the ability of BMDC cells to prime naive CD8+T cells in vivo[2].
Corticosterone (0.03 or 1 mg/kg; s.c.; single) downregulates expression of BDNF mRNA in dentate gyrus and CA1 of rats[3].
Corticosterone (2.6 mg/kg; in animal feedings; 8 days) restores ethanol intake and preference to approximately normal preoperative levels in adrenalectomy (ADX) rats[4].
| Animal Model: | Adult male Wistar rats (150-170 g; adrenalectomized)[3]. | | Dosage: | 0.03 or 1 mg/kg | | Administration: | Subcutaneous injection; single. | | Result: | Decreased expression of BDNF mRNA in dentate gyrus, with 25% and 50% lower for dosages of 0.03 and 1 mg/kg, respectively (3 h after administration).
Reduced approximately 40% BDNF mRNA level as compared to the t=0 h control group (3 h after administration), but the level increased by 100% when 12 h after administration (compared to t=3 h and t=6 h group). |
| Animal Model: | Male Wistar rats (3-week-old; adrenalectomized)[4]. | | Dosage: | 2.6 mg/kg | | Administration: | In animal feedings; 8 days. | | Result: | Restored ethanol intake and preference of adrenalectomy (ADX) rats to approximately normal preoperative levels and to the levels observed in the sham-operated group (SH) rats. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(288.63 mM;Need ultrasonic) Ethanol : 14.29 mg/mL(41.25 mM;Need ultrasonic) H2O : 0.67 mg/mL(1.93 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.8863 mL | 14.4317 mL | 28.8634 mL | | 5 mM | 0.5773 mL | 2.8863 mL | 5.7727 mL | | 10 mM | 0.2886 mL | 1.4432 mL | 2.8863 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： 20%HP-β-CD 5% Cremophor EL Solubility: 5 mg/mL (14.43 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 20%HP-β-CDin saline Solubility: 4 mg/mL (11.55 mM); Suspended solution; Need ultrasonic 3. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.22 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.22 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。 4. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.22 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.22 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。 5. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.22 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.22 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 6. 请依序添加每种溶剂： 0.5%CMC-Na/saline water Solubility: 2 mg/mL (5.77 mM); Suspended solution; Need ultrasonic and warming and heat to 60℃ 7. 请依序添加每种溶剂： 10% EtOH 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1.43 mg/mL (4.13 mM); Clear solution
此方案可获得 ≥ 1.43 mg/mL (4.13 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 EtOH 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。 8. 请依序添加每种溶剂： 10% EtOH 90% (20%SBE-β-CDin saline) Solubility: ≥ 1.43 mg/mL (4.13 mM); Clear solution
此方案可获得 ≥ 1.43 mg/mL (4.13 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 EtOH 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 9. 请依序添加每种溶剂： 10% EtOH 90%corn oil Solubility: ≥ 1.43 mg/mL (4.13 mM); Clear solution
此方案可获得 ≥ 1.43 mg/mL (4.13 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 14.3 mg/mL 的澄清 EtOH 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。
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