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Submit ReviewML 221
Description: Apelin antagonist
Chemical Name: 5-[(4-Nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one
Purity: ≥99% (HPLC)
Biological Activity for ML 221
ML 221 is an 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 for ML 221
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for ML 221
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 3.85 | 10 |
Preparing Stock Solutions for ML 221
The following data is based on the product molecular weight 385.35. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 25.95 mL | 129.75 mL | 259.5 mL |
| 0.5 mM | 5.19 mL | 25.95 mL | 51.9 mL |
| 1 mM | 2.6 mL | 12.98 mL | 25.95 mL |
| 5 mM | 0.52 mL | 2.6 mL | 5.19 mL |
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Product Datasheets for ML 221
References for ML 221
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for ML 221, please let us know.
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Keywords: ML 221, ML 221 supplier, ML221, apelin, receptors, APJ, antagonists, Apelin, Receptors, 4748, Tocris Bioscience
3 Citations for ML 221
Citations are publications that use Tocris products. Selected citations for ML 221 include:
Yang et al (2017) Elabela/Toddler is an endogenous agonist of the apelin APJ receptor in the adult cardiovascular system, and exogenous administration of the peptide compensates for the downregulation of its expression in pulmonary arterial hypertension. Circulation 135 1160 PMID: 28137936
Pawel et al (2021) Anti-Apoptotic Effect of Apelin in Human Placenta: Studies on BeWo Cells and Villous Explants from Third-Trimester Human Pregnancy. Int J Mol Sci 22 PMID: 33803239
Hall et al (2017) Inhibition of the apelin/apelin receptor axis decreases cholangiocarcinoma growth. Cancer Lett 386 179 PMID: 27894959
Do you know of a great paper that uses ML 221 from Tocris? Please let us know.
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