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MedKoo Cat#: 555644 | Name: AER-271
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

AER-271 is a potent aquaporin-4 ( AER-271 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.

Chemical Structure

AER-271
AER-271
CAS#634913-39-6

Theoretical Analysis

MedKoo Cat#: 555644

Name: AER-271

CAS#: 634913-39-6

Chemical Formula: C15H9ClF6NO5P

Exact Mass: 462.9811

Molecular Weight: 463.65

Elemental Analysis: C, 38.86; H, 1.96; Cl, 7.65; F, 24.59; N, 3.02; O, 17.25; P, 6.68

Price and Availability

Size Price Availability Quantity
50mg USD 550.00 2 Weeks
100mg USD 950.00 2 Weeks
200mg USD 1,650.00 2 Weeks
500mg USD 2,850.00 2 Weeks
1g USD 3,850.00 2 Weeks
2g USD 6,250.00 2 Weeks
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Related CAS #
No Data
Synonym
AER-271; AER 271; AER271;
IUPAC/Chemical Name
2-{[3,5-Bis(trifluoromethyl) phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate
InChi Key
WSHXPHFIHYXZKC-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H9ClF6NO5P/c16-9-1-2-12(28-29(25,26)27)11(6-9)13(24)23-10-4-7(14(17,18)19)3-8(5-10)15(20,21)22/h1-6H,(H,23,24)(H2,25,26,27)
SMILES Code
O=P(O)(OC1=CC=C(Cl)C=C1C(NC2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)=O)O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
AER-271, a phosphonate prodrug derivative of AER-270, is an aquaporin-4 (AQP4) inhibitor.
In vitro activity:
TBD
In vivo activity:
At 3 h post-CA %BW was increased in CA-vehicle-treated vs. naive rats (83.84 [83.16, 83.39]) vs. 83.17 [82.68, 83.28] respectively, p<0.05) (Figure 2a). AER-271 treatment prevented the acute increase in %BW (83.29 [83.16, 83.39], CA-AER-271 vs naïve NS) and reduced the amount of edema present at 3 h by 82.1%, returning %BW nearly to the naïve value. %BW in the injury cohorts decreased towards levels of naïve rats at 6 h and 24 h post-CA (Figure 2b-c). Reference: Pediatr Res. 2019 Mar; 85(4): 511–517. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6397683/
Solvent mg/mL mM comments
Solubility
DMSO 125.0 269.60
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 463.65 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Wallisch JS, Janesko-Feldman K, Alexander H, Jha RM, Farr GW, McGuirk PR, Kline AE, Jackson TC, Pelletier MF, Clark RSB, Kochanek PM, Manole MD. 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. Epub 2018 Oct 26. PMID: 30367162; PMCID: PMC6397683.
In vitro protocol:
TBD
In vivo protocol:
1. Wallisch JS, Janesko-Feldman K, Alexander H, Jha RM, Farr GW, McGuirk PR, Kline AE, Jackson TC, Pelletier MF, Clark RSB, Kochanek PM, Manole MD. 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. Epub 2018 Oct 26. PMID: 30367162; PMCID: PMC6397683.
1: Wallisch JS, Janesko-Feldman K, Alexander H, Jha RM, Farr GW, McGuirk PR, Kline AE, Jackson TC, Pelletier MF, Clark RSB, Kochanek PM, Manole MD. 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. Epub 2018 Oct 26. PMID: 30367162; PMCID: PMC6397683. 2: Shangzu Z, Dingxiong X, ChengJun M, Yan C, Yangyang L, Zhiwei L, Ting Z, Zhiming M, Yiming Z, Liying Z, Yongqi L. Aquaporins: Important players in the cardiovascular pathophysiology. Pharmacol Res. 2022 Sep;183:106363. doi: 10.1016/j.phrs.2022.106363. Epub 2022 Jul 26. PMID: 35905892. 3: Kochanek PM, Bramlett HM, Dixon CE, Dietrich WD, Mondello S, Wang KKW, Hayes RL, Lafrenaye A, Povlishock JT, Tortella FC, Poloyac SM, Empey P, Shear DA. Operation Brain Trauma Therapy: 2016 Update. Mil Med. 2018 Mar 1;183(suppl_1):303-312. doi: 10.1093/milmed/usx184. PMID: 29635589. 4: Kochanek PM, Bramlett HM, Shear DA, Dixon CE, Mondello S, Dietrich WD, Hayes RL, Wang KK, Poloyac SM, Empey PE, Povlishock JT, Mountney A, Browning M, Deng- Bryant Y, Yan HQ, Jackson TC, Catania M, Glushakova O, Richieri SP, Tortella FC. Synthesis of Findings, Current Investigations, and Future Directions: Operation Brain Trauma Therapy. J Neurotrauma. 2016 Mar 15;33(6):606-14. doi: 10.1089/neu.2015.4133. PMID: 26671284. 5: Farr GW, Hall CH, Farr SM, Wade R, Detzel JM, Adams AG, Buch JM, Beahm DL, Flask CA, Xu K, LaManna JC, McGuirk PR, Boron WF, Pelletier MF. 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. Epub 2019 Feb 7. PMID: 30738082; PMCID: PMC6495193.