ML 221

Pricing Availability   Qty
Description: Apelin antagonist
Chemical Name: 5-[(4-Nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one
Purity: ≥99% (HPLC)
Citations (3)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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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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:

Hall et al (2017) Inhibition of the apelin/apelin receptor axis decreases cholangiocarcinoma growth. Cancer Lett 386 179 PMID: 27894959

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

Do you know of a great paper that uses ML 221 from Tocris? Please let us know.

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