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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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AER-271 is a novel and potent aquaporin-4 (AQP4) inhibitor that blocks acute cerebral edema and improves early outcome in a pediatric model of asphyxial cardiac arrest. Treatment with AER-271 ameliorated early cerebral edema measured at 3 h after CA vs vehicle treated rats. This treatment also attenuated early NDS. In contrast to rats treated with vehicle after CA, rats treated with AER-271 did not develop significant neuronal death or neuroinflammation as compared to sham.
| ln Vivo |
In vivo, endogenous phosphatases change AER-271 into AER-270. In a juvenile model of wild-type respiratory cardiac arrest, AER-271 causes cerebral edema and enhances early outcomes [1]. In an emergency animal model of cerebral stroke, AER-271 improves neurological outcomes and decreases cerebral edema. In a localized stroke model, administration of AER-271 (5 mg/kg; i.p.) resulted in better outcomes and decreased cerebral edema [2].
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| Animal Protocol |
Animal/Disease Models: Male mice (C57BL/6J, 8-12 weeks old, 25- 30 g) [2]
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection Treatment Experimental Results: Good effect, mean neurological score of 0.89 Compared with control mice receiving vehicle, mean neurological score of ±0.31 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. |
| Molecular Formula |
C15H9CLF6NO5P
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|---|---|
| Molecular Weight |
463.6532
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| Exact Mass |
462.9811
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| Elemental Analysis |
C, 38.86 H, 1.96 Cl, 7.65 F, 24.59 N, 3.02 O, 17.25 P, 6.68
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| CAS # |
634913-39-6
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| SMILES |
ClC1C([H])=C([H])C(=C(C=1[H])C(N([H])C1C([H])=C(C(F)(F)F)C([H])=C(C(F)(F)F)C=1[H])=O)OP(=O)(O[H])O[H]
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| Chemical Name |
2-{[3,5-Bis(trifluoromethyl) phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate
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| Synonyms |
AER 271 AER-271 AER271
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~269.60 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.49 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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