Indomethacin (Indometacin) sodium hydrateis 是一种有效的口服活性COX1/2抑制剂，COX-1 和 COX-2 的IC50值分别为 18 nM 和 26 nM。Indomethacin sodium hydrateis 具有抗癌和抗感染活性。Indomethacin sodium hydrateis 可用于癌症、炎症和病毒感染的研究。
| 生物活性 | Indomethacin (Indometacin) sodium hydrateis a potent, orally activeCOX1/2inhibitor withIC50values of 18 nM and 26 nM forCOX-1andCOX-2, respectively. Indomethacin sodium hydrateis has anticancer activity and anti-infective activity. Indomethacin sodium hydrateis can be used forcancer, inflammation and viralinfectionresearch[1][2][3]. |
体外研究
(In Vitro) | Indomethacin (Indometacin) sodium hydrateis (0-150 μM; 24 hours; 3LL-D122 cells) has anticancer activity in vitro[2].
Indomethacin (Indometacin) sodium hydrateis (0-1000 μM) protects the host cells from damage caused by the virus through activates PKR, resulting in elF2α phosphorylation, and in turn shutting of translation of viral protein and inhibiting replication of the virus (IC50=2 μM)[3].
Cell Viability Assay[2] | Cell Line: | 3LL-D122 cells (highly metastatic variant of mouse LLcarcinoma cells) | | Concentration: | 0, 20, 50, 100 and 150μM | | Incubation Time: | 24 hours | | Result: | Inhibited cell viability at 20 mM, with 50% inhibition at 60 mM. |
Cell Cycle Analysis[2] | Cell Line: | 3LL-D122 cells (highly metastatic variant of mouse LLcarcinoma cells) | | Concentration: | 0, 30 and 80μM | | Incubation Time: | 24 hours | | Result: | Decreased in the percentage of cells at the G2/M phase and increased in the percentage of cells at G1 phase. |
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体内研究
(In Vivo) | Indomethacin (Indometacin) sodium hydrateis (0.01-10 mg/kg; p.o.; for 3 hours; male Sprague-Dawley rats) induces paw oedema and hyperalgesmeasurement dose-dependently reversed carrageenan-induced hyperalgesia[1].
Indomethacin (Indometacin) sodium hydrateis (10 mg/mL; p.o.; daily, for 29 days; male C57BL/6J mice) inhibits tumor growth in vivo[2].
| Animal Model: | Male Sprague-Dawley rats[1] | | Dosage: | 0.01-10 mg/kg | | Administration: | Oral administration; for 3 hours | | Result: | Inhibited the carrageenan-induced rat paw oedema (ED50=2.0 mg/kg) and hyperalgesia (ED50=1.5 mg/kg) in a dose-dependent manner. |
| Animal Model: | Male C57BL/6J mice[2] | | Dosage: | 10 mg/mL | | Administration: | Oral administration; daily, for 29 days | | Result: | Delayed the onset of tumor growth and the initial growth rate of the footpad tumors. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |
| 溶解性数据 | In Vitro: H2O : 25 mg/mL(57.63 mM;Need ultrasonic) DMSO : 12.5 mg/mL(28.81 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.3051 mL | 11.5255 mL | 23.0510 mL | | 5 mM | 0.4610 mL | 2.3051 mL | 4.6102 mL | | 10 mM | 0.2305 mL | 1.1526 mL | 2.3051 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 (protect from light, stored under nitrogen)。-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： PBS Solubility: 5 mg/mL (11.53 mM); Clear solution; Need ultrasonic and warming and heat to 60℃ 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.79 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.79 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。 *以上所有助溶剂都可在本网站选购。
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