ML 221

Catalog #: 4748
3 Citations Datasheet / COA / SDS

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ML 221 | CAS No. 877636-42-5 | Apelin Receptor Antagonists

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Description: Apelin antagonist

Chemical Name: 5-[(4-Nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one

Purity: ≥99%

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Product Details

Citations (3)

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Biological Activity

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

M.Wt:

385.35

Formula:

C₁₇H₁₁N₃O₆S

Solubility:

Soluble to 10 mM in DMSO

Purity:

≥99%

Storage:

Store at +4°C

CAS No:

877636-42-5

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.

Background References

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.
Bioorg.Med.Chem.Lett., 2012;22:6656

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Citations for ML 221

The citations listed below are publications that use Tocris products. Selected citations for ML 221 include:

3 Citations: Showing 1 - 3

Anti-Apoptotic Effect of Apelin in Human Placenta: Studies on BeWo Cells and Villous Explants from Third-Trimester Human Pregnancy.
Authors: Pawel Et al.
Int J Mol Sci 2021;22
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.
Circulation 2017;135:1160

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