Biological Activity
Selective endothelial lipase (EL) inhibitor (IC50 = 237 nM for human EL). Exhibits >20-fold selectivity for EL over lipoprotein lipase (LPL) and hepatic lipase (HL). Increases high density lipoprotein cholesterol (HDLc) plasma levels in mice. Orally bioavailable.
Technical Data
| M. Wt | 366.33 |
| Formula | C18H17F3N2O3 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1515856-92-4 |
| PubChem ID | 72736173 |
| InChI Key | NBGRERFNOKZQLO-AWEZNQCLSA-N |
| Smiles | OC(C1=C(N2CC[C@H](OCC3=CC=CC=N3)C2)C=CC(C(F)(F)F)=C1)=O |
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 | 36.63 | 100 | |
| ethanol | 36.63 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 366.33. 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 | 2.73 mL | 13.65 mL | 27.3 mL |
| 5 mM | 0.55 mL | 2.73 mL | 5.46 mL |
| 10 mM | 0.27 mL | 1.36 mL | 2.73 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.55 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Sun et al (2013) Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice. Bioorg.Med.Chem. 21 7724 PMID: 24211162
Keywords: XEN 445, supplier, XEN445, Selective, endothelial, lipase, EL, inhibitors, inhibits, orally, bioavailable, Lipases, Lipases, Tocris Bioscience
