ML221

  Cat. No.:  DC10793   Featured
Chemical Structure
877636-42-5
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More than 5000 active chemicals with high quality for research!
Field of application
ML221 is an antagonist of the apelin (APJ) receptor.
Cas No.: 877636-42-5
Chemical Name: [4-oxo-6-(pyrimidin-2-ylsulfanylmethyl)pyran-3-yl] 4-nitrobenzoate
Synonyms: ML221; ML 221; ML-221
SMILES: O=C(OC1=COC(CSC2=NC=CC=N2)=CC1=O)C3=CC=C([N+]([O-])=O)C=C3
Formula: C17H11N3O6S
M.Wt: 385.35
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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.
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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