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ML221

Chemical Structure : ML221

CAS No.: 877636-42-5

ML221 (ML 221)

Catalog No.: PC-63277Not For Human Use, Lab Use Only.

ML221 is a potent, selective, functional antagonist of apelin receptor (APJ) with IC50 of 1.75 uM in the β-arrestin assay, >37-fold selective over the closely related AT1 receptor.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

ML221 is a potent, selective, functional antagonist of apelin receptor (APJ) with IC50 of 1.75 uM in the β-arrestin assay, >37-fold selective over the closely related AT1 receptor.
ML221 inhibits apelin-13-mediated activation of APJ in cAMP assays with IC50 of 0.7 uM.
ML221 inhibits cholangiocarcinoma proliferation and angiogenesis, significantly decreases tumor growth in nu/nu mice.

Physicochemical Properties

M.Wt 385.35
Formula C17H11N3O6S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Maloney PR, et al. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6656-60.

2. Sakamoto K, et al. Eur J Pharmacol. 2016 Nov 15;791:213-220.

3. Ishimaru Y, et al. Sci Rep. 2017 Nov 8;7(1):15062.

4. Hall C, et al. Cancer Lett. 2017 Feb 1;386:179-188.

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