| Identification | Back Directory | [Name]
5-[(4-Nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one | [CAS]
877636-42-5 | [Synonyms]
ML221
CS-2842
ML 221;ML-221
ML221 >=98% (HPLC)
ML221; ML 221; ML-221
5-[(4-Nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one
4H-Pyran-4-one, 5-[(4-nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]- | [Molecular Formula]
C17H11N3O6S | [MOL File]
877636-42-5.mol | [Molecular Weight]
385.35 |
| Chemical Properties | Back Directory | [Boiling point ]
624.1±55.0 °C(Predicted) | [density ]
1.54±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO: soluble5mg/mL, clear (warmed) | [form ]
powder | [pka]
0.30±0.33(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Description]
ML-221 is an antagonist of the G protein-coupled receptor (GPCR) APJ (IC50 = 4.8 μM). 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. 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. ML-221 also inhibits pathological angiogenesis and enhances normal vessel recovery in retinal ischemic regions in a mouse model of oxygen-induced retinopathy. | [Uses]
ML 221 is a functional antagonist of the apelin (APJ) receptor which is shown to treat or mediate the homeostasis of the cardiovascular system. | [Definition]
ChEBI: 4-nitrobenzoic acid [4-oxo-6-[(2-pyrimidinylthio)methyl]-3-pyranyl] ester is a nitrobenzoic acid. | [storage]
Store at +4°C |
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| Company Name: |
Twochem Co.Ltd.
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| Tel: |
021-58111628 15800915896 |
| Website: |
http://cn.twochem.com |
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