ML221
ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
Product Specifications
CAS Number
[877636-42-5]
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Apelin Receptor (APJ) ; Arrestin
Type
Reference compound
Related Pathways
GPCR/G Protein
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/ML221.html
Concentration
10mM
Purity
99.01
Solubility
DMSO : ≥ 31 mg/mL
Smiles
O=C1C=C(CSC2=NC=CC=N2)OC=C1OC(C3=CC=C([N+]([O-])=O)C=C3)=O
Molecular Formula
C17H11N3O6S
Molecular Weight
385.35
Precautions
H302, H315, H319, H335
References & Citations
[1]Maloney PR, et al. 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. 2012 Nov 1;22 (21) :6656-60.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
Curated Selection
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