| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Peretinoin primarily targets nuclear retinoic acid receptors (RARs), which are ligand-activated transcription factors. By binding to and activating RARs, Peretinoin modulates the expression of genes involved in the regulation of cell proliferation, cell differentiation, and apoptosis. It also downregulates sphingosine kinase 1 (SPHK1) by reducing the transcription factor Sp1. Peretinoin activates the autophagy pathway by increasing Atg16L1 expression.
|
|---|---|
| ln Vitro |
Even at 10 μM, peretinoin (10–40 μM; 12-72 hours) demonstrated suppressed SPHK1 expression after 24 hours of treatment; this effect became more pronounced after 72 hours [1]. promotes autophagy corrosion and upregulates the expression of LC3B-II in mouse primary hepatocytes [2]. Assay for Cell Autophagy[2]
In vitro, Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) by downregulating the transcription factor Sp1. It prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with an EC50 of 9 μM. |
| ln Vivo |
In vivo, Peretinoin has shown promising results in clinical trials for the prevention and treatment of various cancers. It exerts its anticancer effects by inducing cell differentiation, inhibiting cell proliferation, and promoting apoptosis. It has been studied for the prevention of hepatocellular carcinoma (HCC) and the treatment of non-alcoholic steatohepatitis (NASH). Its oral availability makes it suitable for long-term chemoprevention studies.
|
| Enzyme Assay |
The in vitro activity of Peretinoin is assessed using cell-based RAR activation assays. Cells transfected with an RAR-responsive reporter gene are treated with various concentrations of Peretinoin, and reporter gene activity is measured. For SPHK1 studies, cells are treated with Peretinoin, and SPHK1 mRNA levels are measured by qPCR. For autophagy studies, cells are treated with Peretinoin, and autophagy markers (e.g., LC3-II, Atg16L1) are analyzed by Western blotting. For HCV studies, HCV replicon cells are treated with Peretinoin.
|
| Cell Assay |
Cell Autophagy Assay[2]
Cell Types: Mouse primary hepatocytes (MPH) and human HCC HepG2 cell line Tested Concentrations: 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Upregulates the expression of LC3B-II and increases autophagy flux. Western Blot Analysis[1] Cell Types: Human liver cancer (Huh-7) Cell Tested Concentrations: 10, 20 and 40 μM Incubation Duration: 12, 24, 48 and 72 hrs (hours) Experimental Results: After 24 hrs (hours) of treatment, SPHK1 expression was inhibited, even after 10 microns. For cellular assays, various cancer cell lines or primary cells are cultured in appropriate media. Cells are treated with various concentrations of Peretinoin (typically 0.1-100 µM) for defined periods (24-72 hours). Cell viability is assessed using MTT or CellTiter-Glo assays. Apoptosis is evaluated by flow cytometry using Annexin V/PI staining. The expression of RAR target genes, SPHK1, and autophagy markers is analyzed by Western blotting or qPCR. Cell cycle analysis is performed by flow cytometry. |
| Animal Protocol |
In vivo, Peretinoin is typically administered orally to animal models or patients. In preclinical studies, the compound is administered at various doses (typically 1-100 mg/kg) daily for several weeks. In clinical trials, it is administered orally at doses ranging from 10-100 mg. Efficacy is assessed by measuring tumor growth, disease progression, and survival. In NASH models, liver histology and markers of inflammation and fibrosis are assessed.
|
| ADME/Pharmacokinetics |
Peretinoin has a molecular weight of 302.45 g/mol and a molecular formula of C20H30O2. It is soluble in DMSO at 10 mM. The compound should be stored as a powder at -20°C, protected from light and stored under nitrogen. It has a logP of 6.9. Specific pharmacokinetic parameters such as bioavailability and half-life are not detailed in the provided search results.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for Peretinoin is not detailed in the provided search results. As a retinoid, it may have side effects similar to other retinoids, including skin dryness, mucous membrane irritation, and potential teratogenicity. The compound is intended for research and clinical use under appropriate regulatory oversight. Comprehensive toxicological studies are required to establish its full safety profile. Standard laboratory safety precautions should be followed when handling the compound.
|
| References |
|
| Additional Infomation |
Perettino is an orally administered, noncyclic retinoid with potential antitumor and chemopreventive activities. Perettino binds to and activates the nuclear retinoic acid receptor (RAR), thereby recruiting co-activating proteins and co-promoting the transcription of target genes with other transcriptional complexes. Therefore, this drug may regulate gene expression involved in the regulation of proliferation, differentiation, and apoptosis in both normal and tumor cells.
Peretinoin is an orally available acyclic retinoid with potential antineoplastic and chemopreventive activities. It has been studied for the prevention of hepatocellular carcinoma (HCC) and the treatment of non-alcoholic steatohepatitis (NASH). Its mechanism involves RAR activation, SPHK1 downregulation, and autophagy activation. Peretinoin has shown promising results in clinical trials for the prevention and treatment of various cancers. It is not approved for clinical use in many regions but is available for research purposes. |
| Molecular Formula |
C20H30O2
|
|---|---|
| Molecular Weight |
302.451006412506
|
| Exact Mass |
302.225
|
| CAS # |
81485-25-8
|
| PubChem CID |
6437836
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
5.992
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
22
|
| Complexity |
496
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(=CCC/C(=C/CC/C(=C/C=C/C(=C/C(=O)O)/C)/C)/C)C
|
| InChi Key |
UUBHZHZSIKRVIV-KCXSXWJSSA-N
|
| InChi Code |
InChI=1S/C20H30O2/c1-16(2)9-6-10-17(3)11-7-12-18(4)13-8-14-19(5)15-20(21)22/h8-9,11,13-15H,6-7,10,12H2,1-5H3,(H,21,22)/b14-8+,17-11+,18-13+,19-15+
|
| Chemical Name |
(2E,4E,6E,10E)-3,7,11,15-tetramethylhexadeca-2,4,6,10,14-pentaenoic acid
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~165.32 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.27 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 25.0 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: 2.5 mg/mL (8.27 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3063 mL | 16.5317 mL | 33.0633 mL | |
| 5 mM | 0.6613 mL | 3.3063 mL | 6.6127 mL | |
| 10 mM | 0.3306 mL | 1.6532 mL | 3.3063 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.
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
