| 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 | [InChIKey]
WSHXPHFIHYXZKC-UHFFFAOYSA-N | [SMILES]
FC(F)(F)c1cc(cc(c1)C(F)(F)F)NC(=O)c2c(ccc(c2)Cl)O[P](=O)(O)O |
| Hazard Information | Back Directory | [Uses]
AER-271, a phosphonate proagent derivative of AER-270, is an aquaporin-4 (AQP4) inhibitor for the research of acute ischemic stroke[1]. | [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). | [in vivo]
AER-271 is converted in vivo to AER-270 by endogenous phosphatases. AER-271 blocks acute cerebral edema and improves early outcome in a pediatric model of asphyxial cardiac arrest[1].
AER-271 reduces cerebral edema and improves neurological outcomes in rodent ischemic stroke models. Mice treated with AER-271 (5 mg/kg; i.p. injection) show improved outcomes and reduced cerebral edema in a model of ischemic stroke[2]. | Animal Model: | Male mice (C57BL/6J, 8-12?week-old, 25-30?g)[2] | | Dosage: | 5?mg/kg | | Administration: | Treated by i.p. injection | | Result: | Had better outcomes with an average neurological score of 0.89±0.31 compared with control mice receiving vehicle had an average neurological score of 2.50±0.62. |
| [References]
[1] Wallisch JS, et al. The aquaporin-4 inhibitor AER-271 blocks acute cerebral edema and improves early outcome in a pediatric model of asphyxial cardiac arrest. Pediatr Res. 2019 Mar;85(4):511-517. DOI:10.1038/s41390-018-0215-5
[2] Farr GW, et al. Functionalized Phenylbenzamides Inhibit Aquaporin-4 Reducing Cerebral Edema and Improving Outcome in Two Models of CNS Injury. Neuroscience. 2019 Apr 15;404:484-498. DOI:10.1016/j.neuroscience.2019.01.034 |
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