Biological Activity
Apelin receptor (APJ) antagonist (IC50 values are 0.70 and 1.75 μM in a cAMP assay and β-arrestin assay, respectively). Displays >37-fold selectivity over the closely related angiotensin II type 1 (AT1) receptor. Exhibits no toxicity towards human hepatocytes at concentrations >50 μM.
Technical Data
| M. Wt | 385.35 |
| Formula | C17H11N3O6S |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 877636-42-5 |
| PubChem ID | 7217941 |
| InChI Key | UASIRTUMPRQVFY-UHFFFAOYSA-N |
| Smiles | O=C(C3=CC=C([N+]([O-])=O)C=C3)OC1=COC(CSC2=NC=CC=N2)=CC1=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 | 3.85 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 385.35. 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 | 2.6 mL | 12.98 mL | 25.95 mL |
| 5 mM | 0.52 mL | 2.6 mL | 5.19 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.6 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Maloney et al (2012) Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor. Bioorg.Med.Chem.Lett. 22 6656 PMID: 23010269
Keywords: ML 221, supplier, ML221, apelin, receptors, APJ, antagonists, Apelin, Receptors, Apelin, Receptors, Tocris Bioscience
