1. Immunology/Inflammation
    Autophagy
    Anti-infection
  2. COX
    Autophagy
    Bacterial
  3. Indomethacin

Indomethacin (Synonyms: Indometacin)

Cat. No.: HY-14397 Purity: 99.97%
Handling Instructions

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. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.

For research use only. We do not sell to patients.

Indomethacin Chemical Structure

Indomethacin Chemical Structure

CAS No. : 53-86-1

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Customer Review

Based on 9 publication(s) in Google Scholar

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Description

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].

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].

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

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[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].

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

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

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

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

  • 4.

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

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

  • 5.

    Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in saline)

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

  • 6.

    Add each solvent one by one:  10% EtOH    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
Animal Administration
[3]

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].

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

References
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Keywords:

IndomethacinIndometacinCOXAutophagyBacterialCyclooxygenaseCOX1COX2autophagicfluxlysosomeNon-steroidalanti-inflammatoryNSAIDInhibitorinhibitorinhibit

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Indomethacin
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