Biological Activity
Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor (IC50 = 0.18 μM). Exhibits hypocholesterolaemic and antiatherosclerotic activity in vivo.
Licensing Information
Sold with the permission of Astellas Pharma Inc.
Technical Data
| M. Wt | 452.63 |
| Formula | C31H36N2O |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 138046-43-2 |
| PubChem ID | 9911716 |
| InChI Key | FMLJREWZCZHGGW-UHFFFAOYSA-N |
| Smiles | O=C(NC5=C(C)C=C(C)C=C5C)N(C4CCCCCC4)CC3=CC2=C(C=C3)C1=CC=CC=C1C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.26 | 100 | |
| ethanol | 4.53 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 452.63. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.21 mL | 11.05 mL | 22.09 mL |
| 5 mM | 0.44 mL | 2.21 mL | 4.42 mL |
| 10 mM | 0.22 mL | 1.1 mL | 2.21 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Nagata et al (1995) N-[2-[N'-pentyl-(6,6-dimethyl-2,4-heptadiynyl)amino]ethyl]-(2-methyl-1-naphthylthio)acetamide (FY-087). A new acyl coenzyme A: cholesterol acyltransferase (ACAT) inhibitor of diet-induced atherosclerosis formation in mice. Biochem.Pharmacol. 49 643 PMID: 7887979
Kamiya et al (2000) Bioavailable acyl-CoA: cholesterol acyltransferase inhibitor with anti-peroxidative activity: synthesis and biological activity of novel indolinyl amide and urea derivatives. Chem.Pharm.Bull. 48 817 PMID: 10866142
Miike et al (2008) Effects of an anti-oxidative ACAT inhibitor on apoptosis/necrosis and cholesterol accumulation under oxidative stress in THP-1 cell dervied foam cells. Life Sci. 82 79 PMID: 18037448
Keywords: YM 750, supplier, Acyl-CoA:cholesterol, acyltransferase, ACAT, inhibitors, inhibits, transferase, YM750, Acyl-CoA:Cholesterol, Acyltransferase, Acyl-CoA:Cholesterol, Acyltransferase, Tocris Bioscience
