ML 221

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

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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 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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References

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

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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