ML-221, CAS 877636-42-5

Formulation: A crystalline solid

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

Purity: ≥98%

Formula Markup: C17H11N3O6S

Formula Weight: 385,4

Shelf life (days): 1460

CAS Number: 877636-42-5

Notes: 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}

• SKU: CAY27313-25
• Manufacturer: Cayman Chemical
• Manufacturer SKU: 27313-25
• Green Labware: No
• Package Unit: 25 mg
• Quantity Unit: STK