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Indomethacin COX Inhibidor

Cat. No.: S1723

Indomethacin es un inhibidor no selectivo de COX1 y COX2 con IC50 de 0,1 μg/mL y 5 μg/mL, respectivamente, utilizado para reducir la fiebre, el dolor, la rigidez y la hinchazón.
Indomethacin COX Inhibidor Chemical Structure

Estructura química

Peso molecular: 357.79

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Control de calidad (Quality Control)

Lote: Pureza: 100.00%
100.00

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares Tipo de ensayo Concentración Tiempo de incubación Formulación Descripción de la actividad PMID
HeLa cells Function assay 20 mins Agonist activity at androgen receptor (unknown origin) expressed in HeLa cells co-expressing PSA-(ARE)4-Luc13 assessed as induction of DHT-induced luciferase activity after 20 mins by luciferase reporter gene assay, EC50=0.14 nM
J774 cells Function assay In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells, IC50=2 nM
U-937 cells Function assay In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells, IC50=2 nM
rat synovial cells Function assay In vitro inhibitory effect on production of prostaglandin E2 (PGE2) in rat synovial cells, IC50=2.9 nM
143982 cells Function assay In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (COX-2) in 143982 cells, IC50=9 nM
CHO cells Function assay In vitro inhibitory potency against human COX-1 in stably transfected chinese hamster ovary (CHO) cells, IC50=18 nM
RBL-1 cell line Function assay Inhibition of Prostaglandin G/H synthase in intact RBL-1 cell line, IC50=0.5 μM
SF-9 insect cells Function assay 20 Mins Inhibition of human COX2 expressed in SF-9 insect cells assessed as conversion of [14C]-arachidonic acid to [14C]-prostaglandins preincubated for 20 mins by thin-layer chromatography analysis, IC50=0.75 μM
mouse RAW264.7 cells Function assay 24 h Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess assay, IC50=1.25 μM
mouse BV2 cells Function assay 24 h Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess assay, IC50=7.1 μM
human 2008 cells Function assay Inhibition of human MRP1 in human 2008 cells, IC50=12 μM
A549 cells  Function assay 10 μM Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation at 10 uM by cell-intact assay
HepG2 cells Function assay 100 μM Inhibition of MRP1-mediated doxorubicin efflux in doxorubicin resistant human HepG2 cells at 100 uM by flow cytometry
THP1 cells Function assay 100 μM 30 mins Irreversible inhibition of COX-1 in human THP1 cells assessed as inhibition of arachidonic acid-induced TXB2 formation at 100 uM incubated for 30 mins followed by compound washout measured 30 mins post arachidonic acid challenge by radioimmunoassay
MDA-MB-231 cells Function assay 100 μM 30 mins Irreversible inhibition of COX-1 in human MDA-MB-231 cells assessed as inhibition of arachidonic acid-induced PGE2 formation at 100 uM incubated for 30 mins followed by compound washout measured 30 mins post arachidonic acid challenge by radioimmunoassay
LNCAP cells Function assay 30 μM 48 h Inhibition of AKR1C3 (unknown origin)-mediated testosterone-17beta-glucuronide formation expressed in human LNCAP cells at 30 uM after 48 hrs in presence of 4-androstene-3,17-dione
mouse BV2 cells Cytotoxicity assay 24 h Cytotoxicity against mouse BV2 cells assessed as maximum non-toxic concentration after 24 hrs by MTT assay
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular 357.79 Fórmula

C19H16ClNO4

 Almacenamiento (Desde la fecha de recepción)
Nº CAS 53-86-1 Descargar SDF Almacenamiento de soluciones madre

Sinónimos Indometacin,NSC-77541 Smiles CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)O

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 72 mg/mL (201.23 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 24 mg/mL

Water : Insoluble

Calculadora de Molaridad

Masa Concentración Volumen Peso molecular
Calculadora de Dilución Calculadora de Peso Molecular

In vivo
Lote:

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

mg/kg g μL

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH2O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Targets/IC50/Ki
COX1
0.28 μM
COX-2
14 μM
In vitro
Indomethacin inhibits transcription of a beta-catenin/TCF-responsive reporter gene in a dose dependent manner. This compound also downregulates the beta-catenin/TCF transcriptional target cyclin D1. It attenuates the transcription of beta-catenin/TCF-responsive genes, by modulating TCF activity without disrupting beta-catenin/TCF complex formation.
In vivo
Indomethacin increases BrdU+ cells of all lineages and reduces microglial/monocyte activation in rats after focal cerebral ischemia. This compound (7.5 mg/kg, one injection) produces acute injury and inflammation in the distal jejunum and proximal ileum that are maximal at three days and completely resolves within one week. It (two daily subcutaneous injections) produces a more extensive and chronic inflammation that lasts in an active form in more than 75% of the rats for at least two weeks. This chemical (4ppm) reduces tumor yield by 78% in SKH:HR-1-hrBr hairless mice. It (20 mg/kg, orally) increases the total area of gastric erosions and concentration of lipid peroxides in the gastric mucosa of rats. This compound increases the alpha-tocopherol:total cholesterol ratio in serum. It inhibits the increases in gastric mucosal erosions and lipid peroxides in the gastric mucosa, and the reduction of serum alpha-tocopherol.
Referencias
  • [4] https://pubmed.ncbi.nlm.nih.gov/10449029/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8314503/
  • [6] https://pubmed.ncbi.nlm.nih.gov/8265610/

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT Reclutamiento Condiciones Patrocinador/Colaboradores Fecha de inicio Fases
NCT06031363 Completed
Pancreatitis|Cholangiopancreatography Endoscopic Retrograde|Indomethacin
The First Affiliated Hospital of Soochow University
 November 1 2022 Not Applicable
NCT04821323 Completed
Healthy
Janssen Research & Development LLC
 March 10 2021 Early Phase 1
NCT04025177 Withdrawn
Patent Ductus Arteriosus After Premature Birth
University of Manitoba|St. Boniface Hospital|Health Sciences Centre Winnipeg Manitoba|University at Buffalo
 January 2020 Phase 2
NCT03967483 Unknown status
Headache Migraine
Anne Ducros|French Society for the Study of Migraine Headache
 June 1 2019 --