ML221 , 10mMinDMSO , 877636-42-5
Synonym(s):
5-[(4-Nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one
| Pack Size | Price | Stock | Quantity |
| 1ml | RMB384.80 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| 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) |
| pka | 0.30±0.33(Predicted) |
| form | powder |
| color | white to beige |
Description and Uses
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.
ML 221 is a functional antagonist of the apelin (APJ) receptor which is shown to treat or mediate the homeostasis of the cardiovascular system.
Safety
| Symbol(GHS) |  GHS07 |
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
| WGK Germany | 3 |
