Hydrocotarnine 是一种Cbl抑制剂，可导致结肠炎炎症小体介导的 IL-18 分泌。Hydrocotarnine 能增加细胞糖酵解代谢中的 GLUT1 表达和对葡萄糖的摄取。Hydrocotarnine 在癌症研究中具有镇痛作用。
| 生物活性 | Hydrocotarnine is aCblinhibitor, and results in inflammasome-mediatedIL-18secretion in colitis. Hydrocotarnine increases expression ofGLUT1and cellular glucose uptake in glycolytic metabolism. Hydrocotarnine acts as an agent that provides analgesic effect incancerresearch[1][2][3]. |
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体外研究
(In Vitro) | Hydrocotarnine is an analgesic agent (CRIN-2), with the patent ID of WO2011160016A2[1].
Hydrocotarnine (10 μM; 1 h) elevates the secretion of IL-1β and IL-18, and (0.1-10 μM; 1 h) increases the global level of tyrosine-phosphorylated proteins in THP-1 cells[1].
Hydrocotarnine (50 μM; 0-100 min) increases the glycolytic capacity and glycolytic reserve capacity in THP-1-derived macrophages[2].
Hydrocotarnine (50 μM; 16 h) inhibits Cbl and increases the total GLUT1 protein in THP-1-derived macrophages[2].
Hydrocotarnine is known to enhance the analgesic effect of opioids, and alleviates cancer pain[3].
Western Blot Analysis[1] | Cell Line: | THP-1 cells | | Concentration: | 0.1, 1, 10 μM | | Incubation Time: | 1 hour | | Result: | Induced p-Pyk2 loss and increased the level of tyrosine-phosphorylated proteins in a dose-dependent manner. |
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体内研究
(In Vivo) | Hydrocotarnine (10 mg/kg/d; i.p.; 9 d) shows inhibitory effect on Cbl and results in increasing IL-18 levels, indicating that NLRP3 inflammasome activation is enhanced in mice[1].
Hydrocotarnine (10 mg/kg/d; i.p.; 9 d) protects mice from DSS-induced colitis, with low scores of pathological evaluation of inflammation, epithelial defects, and crypt atrophy[1].
| Animal Model: | DSS-induced colitis model in C57BL/6 mice (6-9 weeks old)[1] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection; once daily; 9 days while 2.5% DSS treatment began on day 1 and ended on day 7 | | Result: | Significantly attenuated the weight loss of DSS-induced colitis mice compared to PBS-treated control mice, indicating that decreasing negative regulation of the NLRP3 inflammasome activation could attenuate colitis in an animal model. |
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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(451.98 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 4.5198 mL | 22.5989 mL | 45.1977 mL | | 5 mM | 0.9040 mL | 4.5198 mL | 9.0395 mL | | 10 mM | 0.4520 mL | 2.2599 mL | 4.5198 mL |
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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: ≥ 2.5 mg/mL (11.30 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.30 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (11.30 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.30 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (11.30 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.30 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。 *以上所有助溶剂都可在本网站选购。
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