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1mg |
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5mg |
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10mg |
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50mg |
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100mg |
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Oleoylethanolamide (AM-1301; AM1301) is an endogenous and potent PPAR-α agonist with the potential to be used in the treatment of obesity and arteriosclerosis.
ln Vitro |
Hepatic stellate cells are the target of oléoylethanolamide (OEA), an endogenous PPAR-α ligand that attenuates liver fibrosis. Through PPAR-α, oleoylethanolamide inhibits the activation of hepatic stellate cells (HSCs) elicited by TGF-β1 in vitro. qPCR is used to measure the expression levels of Col1a and α-SMA in TGF-β1-stimulated HSCs in order to evaluate the effect of oleoylethanolamide on HSC activation. When TGF-β1 (5 ng/mL) is stimulated for 48 hours in the group of CFSC cells, the mRNA levels of α-SMA and Col1a are significantly increased; however, the mRNA levels are inhibited in a dose-dependent way when Oleoylethanolamide is applied. The results of immunofluorescence and western blot demonstrate that treatment with oleoylethanolamide dose-dependently suppresses the production of the HSC activation marker α-SMA in protein form. Oleoylethanolamide's inhibitory effects on HSC activation are totally prevented by the PPAR-α antagonist MK886 (10 μM). Furthermore, PPAR-α's mRNA and protein expression levels are down-regulated in response to TGF-β1 stimulation; however, these changes are dose-dependently restored by oleoylethanolamide therapy. Furthermore, it has been discovered that TGF-β1 stimulation causes an upregulation of Smad 2/3 phosphorylation, which is in line with the effects on HSC activation. On the other hand, phosphorylation of Smad 2/3 in CFSC mimicked with TGF-β1 is decreased by oleoylethanolamide (10 μM).
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ln Vivo |
In mice models of hepatic fibrosis, oleoylethanolamide (OEA) can highly reduce the pro-fibrotic cytokine TGF-β1 and adversely regulate genes in the TGF-β1 signaling pathway (α-SMA, collagen 1a, and collagen 3a). By preventing the activation of hepatic stellate cells (HSCs), treatment with oleoylethanolamide (5 mg/kg/day, intraperitoneal injection, ip) considerably slows the progression of liver fibrosis in both experimental animal models[1].
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References |
[1]. Chen L, et al. Oleoylethanolamide, an endogenous PPAR-α ligand, attenuates liver fibrosis targeting hepatic stellate cells. Oncotarget. 2015 Dec 15;6(40):42530-40
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Molecular Formula |
C₂₀H₃₉NO₂
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Molecular Weight |
325.53
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CAS # |
111-58-0
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Related CAS # |
Oleoylethanolamide-d4;946524-36-3;Oleoylethanolamide-d2;1245477-09-1
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SMILES |
CCCCCCCC/C=C\CCCCCCCC(NCCO)=O
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Synonyms |
N-(2-HydroxyethyloleamideAM-1301AM1301 OEA
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~20.83 mg/mL (~63.99 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.0719 mL | 15.3596 mL | 30.7191 mL | |
5 mM | 0.6144 mL | 3.0719 mL | 6.1438 mL | |
10 mM | 0.3072 mL | 1.5360 mL | 3.0719 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.