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  3. Indomethacin

Indomethacin (Synonyms: Indometacin)

目录号: HY-14397 纯度: 99.71%
产品使用指南

Indomethacin 是一种有效的、非选择性的 COX1COX2 抑制剂,在 CHO 细胞中,对人 COX-1 和 COX-2 的 IC50 值分别为 18 nM 和 26 nM。

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Indomethacin Chemical Structure

Indomethacin Chemical Structure

CAS No. : 53-86-1

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10 mM * 1 mL in DMSO ¥500 In-stock
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Description

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.

IC50 & Target[1]

Human COX-1

18 nM (IC50, in CHO cells)

Human COX-2

26 nM (IC50, in CHO cells)

In Vitro

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].

In Vivo

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[2]. Indomethacin (22.9 mg/kg, p.o.) produces 8 to 10 linear mucosal lesions extended from the fundic to pyloric area of stomach wall[3].

Clinical Trial
Molecular Weight

357.79

Formula

C₁₉H₁₆ClNO₄

CAS No.

53-86-1

SMILES

COC1=CC=C(N(C(C2=CC=C(Cl)C=C2)=O)C(C)=C3CC(O)=O)C3=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7949 mL 13.9747 mL 27.9494 mL
5 mM 0.5590 mL 2.7949 mL 5.5899 mL
10 mM 0.2795 mL 1.3975 mL 2.7949 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°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。

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: ≥ 7.5 mg/mL (20.96 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (20.96 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 75.0 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,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: ≥ 2.5 mg/mL (6.99 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.99 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 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,再用生理盐水定溶至 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: ≥ 7.5 mg/mL (20.96 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (20.96 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 75.0 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,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,再用生理盐水定溶至 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。

*以上所有助溶剂都可在 MCE 网站选购。
References
Animal Administration
[2]

Rats[2]
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

IndomethacinIndometacinCOXAutophagyCyclooxygenaseInhibitorinhibitorinhibit

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