Chemical Name: 5-[(4-Nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one
Biological ActivityApelin 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.
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.
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.
Maloney et al.
Citations for ML 221
The citations listed below are publications that use Tocris products. Selected citations for ML 221 include:
2 Citations: Showing 1 - 2
Inhibition of the apelin/apelin receptor axis decreases cholangiocarcinoma growth.
Authors: Hall Et al.
Cancer Lett 2017;386:179
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.
Authors: Yang Et al.
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