research use only
Cat.No.S4708
| Related Targets | Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite |
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| Other PPAR Inhibitors | T0070907 GW9662 GW6471 WY-14643 (Pirinixic Acid) GSK3787 GW0742 AZ6102 Harmine Astaxanthin Eupatilin |
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In vitro |
Ethanol : 59 mg/mL
DMSO
: 5 mg/mL
(16.69 mM)
Water : Insoluble |
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In vivo |
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| Molecular Weight | 299.49 | Formula | C18H37NO2 |
Storage (From the date of receipt) | |
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| CAS No. | 544-31-0 | Download SDF | Storage of Stock Solutions |
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| Synonyms | Palmidrol|N-palmitoylethanolamine | Smiles | CCCCCCCCCCCCCCCC(=O)NCCO | ||
| Targets/IC50/Ki |
PPARα
(In HeLa cells) 3.1 μM(EC50)
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| In vitro |
PEA protects cultured mouse cerebellar granule cells from glutamate toxicity and enhances microglial cell motility. In the mitochondrial fraction from cells stimulated with PEA, steroidogenic acute regulatory protein (StAR) and cytochrome P450 enzyme(P450scc) expression increases, both comprising proteins considered to be involved in crucial steps of neurosteroid formation. Moreover, PEA shows a protective effect, reducing malondialdehyde formation in cells treated with L-buthionine-(S,R)-sulfoximine, a glutathione depletor and the effect of PEA is partially inhibited by finasteride, a 5a-reductase inhibitor.
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| In vivo |
PEA attenuates inflammation in wild-type mice but has no effect in mice deficient in PPAR-α. PEA has been shown to inhibit peripheral inflammation and mast-cell degranulation as well as to exert neuroprotective and antinociceptive effects in rats and mice. These actions are accompanied by changes in nitric oxide production, neutrophil influx, and expression of proinflammatory proteins such as inducible nitric oxide synthase and cyclooxygenase-2. In addition to its known anti-inflammatory activity, PEA regulates many pathophysiological
processes, including pain perception, convulsions, and neurotoxicity. In the central nervous system (CNS), where PEA is present at detectable levels, its concentrations significantly increase under
pathological conditions, such as excitotoxicity, brain ischaemia and neuroinflammation.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06040164 | Not yet recruiting | PreDiabetes|Diabetes Mellitus Type 2|Obesity|Oral Dysbiosis|Mouth Disease |
Fundación Pública Andaluza para la Investigación de Málaga en Biomedicina y Salud |
October 1 2023 | -- |
| NCT05849792 | Completed | Exercise|Physical Fitness|Depression|Adult ALL|Psychological |
University of Cadiz|Consejería de Salud y Familia (Junta de Andalucía)|Institute of Biomedical research and innovation of Cádiz (INIBICA) |
September 1 2019 | Not Applicable |
| NCT03564379 | Completed | Healthy |
Janssen Research & Development LLC |
June 12 2018 | Phase 1 |
| NCT01092845 | Completed | Healthy|Sleep |
Pfizer |
April 2010 | Phase 1 |
| NCT01370720 | Unknown status | Irritable Bowel Syndrome |
MARIA CRISTINA COMELLI|CM&D Pharma Limited |
February 2010 | Phase 2 |
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