Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC₅₀s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells^[1]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes^[2].

Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC₅₀s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin inhibits lipopolysaccharide (LPS)-induced PGE2 production (COX-2) in a human whole blood assay with a potency (IC₅₀=0.68±0.17 μM), and suppresses coagulation-induced TXB2 production (COX-1) (IC₅₀=0.19±0.02 μM). Indomethacin blocks COX-1 with an IC₅₀ of 20±1 nM in U937 cell microsomes at a low arachidonic acid concentration (0.1 μM)^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Indomethacin dose-dependently inhibits both the carrageenan-induced rat paw oedema (ED₅₀, 2.0 mg/kg), hyperalgesia (ED₅₀, 1.5 mg/kg), and is also effective at reversing LPS-induced pyrexia in rats (ED₅₀, 1.1 mg/kg)^[1]. Indomethacin (2.5 mg/kg, i.p) decreases the number of NeuN⁺ cells in the animals at 8 days after ET-1 injection. Indomethacin also reduces microglia/macrophage activation at 14 days. Indomethacin significantly increases the number of SVZ DCX⁺ cells/field at 14 days post stroke^[3]. Indomethacin (22.9 mg/kg, p.o.) produces 8 to 10 linear mucosal lesions extended from the fundic to pyloric area of stomach wall^[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

357.79

C₁₉H₁₆ClNO₄

53-86-1

吲哚美辛

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

DMSO : 100 mg/mL (279.49 mM; Need ultrasonic)

Ethanol : 12.5 mg/mL (34.94 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

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°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 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 (5.81 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.81 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-CD in saline)

  Solubility: ≥ 2.08 mg/mL (5.81 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.81 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 μL 20% 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 (5.81 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.81 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。

• 4.

  请依序添加每种溶剂： 10% EtOH    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 1.25 mg/mL (3.49 mM); Clear solution

  此方案可获得 ≥ 1.25 mg/mL (3.49 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 12.5 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。

  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

• 5.

  请依序添加每种溶剂： 10% EtOH    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 1.25 mg/mL (3.49 mM); Clear solution

  此方案可获得 ≥ 1.25 mg/mL (3.49 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 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
• 6.

  请依序添加每种溶剂： 10% EtOH    90% corn oil

  Solubility: ≥ 1.25 mg/mL (3.49 mM); Clear solution

  此方案可获得 ≥ 1.25 mg/mL (3.49 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 12.5 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Riendeau D, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17.

  [2]. Jorge Vallecillo-Hernández, et al. Indomethacin Disrupts Autophagic Flux by Inducing Lysosomal Dysfunction in Gastric Cancer Cells and Increases Their Sensitivity to Cytotoxic Drugs. Sci Rep. 2018 Feb 26;8(1):3593.

  [3]. Lopes RS, et al. Indomethacin treatment reduces microglia activation and increases numbers of neuroblasts in the subventricular zone and ischaemic striatum after focal ischaemia. J Biosci. 2016 Sep;41(3):381-94.

  [4]. Afroz S, et al. Concentrated phosphatidic acid in cereal brans as potential protective agents against indomethacin-induced stomach ulcer. J Agric Food Chem. 2016 Aug 26.

Rats^[3]
To investigate the effects of Indomethacin treatment on both microglia activation, neuroprotection and adult neurogenesis, rats are divided in four experimental groups: animals injected with ET-1, treated with sterile saline (i.p.) for 7 days and perfused at 8 days following ET-1 injection (group 1, n=4); animals injected with ET-1, treated with Indomethacin (2.5 mg/kg, i.p) for 7 days and perfused at 8 days following ET-1 injection (group 2, n=4); animals injected with ET-1, treated with sterile saline (i.p.) for 7 days and perfused at 14 days following ET-1 injection (group 3, n=4); animals injected with ET-1, treated with Indomethacin (2.5 mg/kg, i.p) for 7 days and perfused at 14 days following ET-1 injection (group 4, n=4). After survival times of 7 or 14 days, animals are deeply anesthetized with a mixture of ketamine hydrochloride (72 mg/kg, i.p.) and xylazine hydrochloride (9 mg/kg, i.p.). After the verification of complete absence of both the corneal and the paw withdraw reflexes, the animals are transcardially perfused with heparinized 0.9% warm phosphate-buffered saline (PBS) followed by 4% cold paraformaldehyde in 0.1 M phosphate buffer (PB), pH 7.4. Brains are post-fixed for 24 h in the same fixative and cryoprotected in different gradients of sucrose-glycerol solutions over 7 days. The tissue is then frozen in an embedding medium, and cut at 30 μM in the coronal plane using a cryostat. Sections are then mounted onto gelatinized slides and stored in a freezer at -20°C^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Riendeau D, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17.

  [2]. Jorge Vallecillo-Hernández, et al. Indomethacin Disrupts Autophagic Flux by Inducing Lysosomal Dysfunction in Gastric Cancer Cells and Increases Their Sensitivity to Cytotoxic Drugs. Sci Rep. 2018 Feb 26;8(1):3593.

  [3]. Lopes RS, et al. Indomethacin treatment reduces microglia activation and increases numbers of neuroblasts in the subventricular zone and ischaemic striatum after focal ischaemia. J Biosci. 2016 Sep;41(3):381-94.

  [4]. Afroz S, et al. Concentrated phosphatidic acid in cereal brans as potential protective agents against indomethacin-induced stomach ulcer. J Agric Food Chem. 2016 Aug 26.