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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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 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|
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
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Keywords: ML 221, ML 221 supplier, ML221, apelin, receptors, APJ, antagonists, Apelin, Receptors, 4748, Tocris Bioscience
2 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
Hall et al (2017) Inhibition of the apelin/apelin receptor axis decreases cholangiocarcinoma growth. Cancer Lett 386 179 PMID: 27894959
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Literature in this Area
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Peptide Hormone Receptors Product ListingUpdated
A collection of over 200 products for peptide hormone receptors, the listing includes research tools for the study of:
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- Blood Pressure Regulation
- Feeding and Appetite Regulation
- Glucose Regulation
- Peptide Hormone Processing