An APJ receptor antagonist (IC50 = 4.8 μM); selective for APJ over AT1 (IC50 = >78 μM); antagonizes apelin 13-induced activation of APJ in cAMP and β-arrestin recruitment assays (IC50s = 0.7 and 1.75 μM

ML-221 – 25 mg

Brand:
Cayman
CAS:
877636-42-5
Storage:
-20
UN-No:
Non-Hazardous - /

ML-221 is an antagonist of the G protein-coupled receptor (GPCR) APJ (IC50 = 4.8 μM).{48358} It is selective for APJ over the angiotensin II type 1 (AT1) receptor (IC50 = >78 μM). ML-221 antagonizes apelin 13-induced activation of APJ in cAMP and β-arrestin recruitment assays (IC50s = 0.7 and 1.75 μM, respectively). It inhibits proliferation and angiogenesis in Mz-ChA-1 cholangiocarcinoma cells when used at concentrations ranging from 5 to 15 μM.{48359} In vivo, ML-221 (150 μg/kg) reduces tumor growth in a Mz-ChA-1 mouse xenograft model. Intrathecal injection of ML-221 (10 μg per animal) reduces mechanical allodynia and heat hyperalgesia induced by chronic constriction injury (CCI) of the sciatic nerve in rats.{48360} ML-221 also inhibits pathological angiogenesis and enhances normal vessel recovery in retinal ischemic regions in a mouse model of oxygen-induced retinopathy.{48361}  

 

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Description

An APJ receptor antagonist (IC50 = 4.8 μM); selective for APJ over AT1 (IC50 = >78 μM); antagonizes apelin 13-induced activation of APJ in cAMP and β-arrestin recruitment assays (IC50s = 0.7 and 1.75 μM, respectively); inhibits proliferation and angiogenesis in Mz-ChA-1 cholangiocarcinoma cells from 5-15 μM; reduces tumor growth in a Mz-ChA-1 mouse xenograft model at 150 μg/kg; reduces sciatic CCI-induced mechanical allodynia and heat hyperalgesia in rats at 10 μg/animal; inhibits pathological angiogenesis and enhances normal vessel recovery in retinal ischemic regions in a mouse model of oxygen-induced retinopathy

Formal name: 5-[(4-nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one

Synonyms: 

Molecular weight: 385.4

CAS: 877636-42-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer|Angiogenesis||Research Area|Neuroscience|Neuroprotection|Ischemia||Research Area|Neuroscience|Ophthalmology||Research Area|Neuroscience|Pain Research

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