Identification | Back Directory | [Name]
AER-271
(AER271) | [CAS]
634913-39-6 | [Synonyms]
AER-271 AER-271
(AER271) Benzamide, N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-(phosphonooxy)- | [Molecular Formula]
C15H9ClF6NO5P | [MDL Number]
MFCD32669785 | [MOL File]
634913-39-6.mol | [Molecular Weight]
463.65 |
Chemical Properties | Back Directory | [density ]
1.692±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMSO:125.0(Max Conc. mg/mL);269.6(Max Conc. mM) | [form ]
Solid | [pka]
0.97±0.50(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Biological Activity]
AER-271 is a phosphonate precursor (prodrug) form of the selective aquaporin 4 (AQP4) inhibitor IMD-0354 (AER-270; hu/m/r IC50 = 420/390/210 nM using respective CHO AQP4 transfectants) with >5000-fold enhanced solubility. AER-271 is rapidly converted to AER-270 in vivo (plasma AER-270 Cmax = 500 ng/mL or 1.75 μM20 min post 10 mg AER-271/kg i.p.; C57BL/6 mice) and exhibits therapeutic efficacy in rodent models of brain damage by cardiac arrest or ischemic stroke (5-10 mg/kg ip. & 0.08 mg/h sc. in mice; 1-10 mg/kg iv. in rats). |
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