图片.png For research use only

Product Infomation
Product NameML221
CAS No.877636-42-5
Molecular Weight

385.35

Formula

C₁₇H₁₁N₃O₆S

SMILES

O=C1C=C(CSC2=NC=CC=N2)OC=C1OC(C3=CC=C([N+]([O-])=O)C=C3)=O

Stock statusGet quote



Online consultation: s_qq.png  s_email.png



Product description

Description

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.



IC50 & Target

________________________________________________________________________________________

IC50: 1.75 μM (APJ, cell-based)[1]


In Vitro

_________________________________________________________________________________________


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. ML221 is >37-fold selective over the closely related angiotensin II type 1 (AT1) receptor (IC50, >79 μM) in cells. ML221 displays limited cross reactivity against a range of GPCRs except the κ-opioid and benzodiazepinone receptors (<50/<70%I at 10 μM)[1].





Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month







Peferences:

 [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.