[CAS NO. 634913-39-6] AER-271
PRODUCTS SPECIFICATIONS [634913-39-6]
DESCRIPTION [634913-39-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 463.65 |
| Molecular Formula | C15H9ClF6NO5P |
| SMILES | O=C(NC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)C2=CC(Cl)=CC=C2OP(O)(O)=O |
Summary
AER-271, a phosphonate prodrug derivative of AER-270, is an aquaporin-4 ( AQP4 ) inhibitor for the research of acute ischemic stroke [1] .
IC50 & 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03804476 | Aeromics, Inc.|Covance |
Stroke|Stroke, Acute|Stroke, Ischemic
|
June 26, 2018 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 269.60 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1568 mL | 10.7840 mL | 21.5680 mL |
| 5 mM | 0.4314 mL | 2.1568 mL | 4.3136 mL |
| 10 mM | 0.2157 mL | 1.0784 mL | 2.1568 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.49 mM); Clear solution
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.