ML 221

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Cat.No. 4748 - ML 221 | C17H11N3O6S | CAS No. 877636-42-5
Description: Apelin receptor (APJ) antagonist
Chemical Name: 5-[(4-Nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

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.

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

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Product Datasheets

Safety Datasheet

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


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Keywords: ML 221, supplier, ML221, apelin, receptors, APJ, antagonists, Apelin, Receptors, Tocris Bioscience

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Literature in this Area

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Pathways for ML 221

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