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AER-271

Names

[ CAS No. ]:
634913-39-6

[ Name ]:
AER-271

[Synonym ]:
2-{[3,5-Bis(trifluoromethyl) phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate

Biological Activity

[Description]:

AER-271, a phosphonate prodrug derivative of AER-270, is an aquaporin-4 (AQP4) inhibitor for the research of acute ischemic stroke[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Others >> Others
Research Areas >> Neurological Disease

[Target]

Aquaporin-4 (AQP4)[1]


[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C15H9ClF6NO5P

[ Molecular Weight ]:
463.653

[ Storage condition ]:
-20°C 12 Months; 4°C 6 Months


Related Compounds

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