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SML2737

AER-271

≥98% (HPLC)

Synonym(s):

2-(3,5-bis(Trifluoromethyl)phenylcarbamoyl)-4-chlorophenyl dihydrogen phosphate, AER-270 phosphate, AER-270 precursor, AER-270 prodrug, IMD-0354 phosphate, IMD-0354 precursor, IMD-0354 prodrug, N-[3,5-bis(Trifluoromethyl)phenyl]-5-chloro-2-(phosphonooxy)benzamide

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About This Item

Empirical Formula (Hill Notation):
C15H9ClF6NO5P
CAS Number:
Molecular Weight:
463.65
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

FC(F)(F)c1cc(cc(c1)C(F)(F)F)NC(=O)c2c(ccc(c2)Cl)O[P](=O)(O)O

InChI key

WSHXPHFIHYXZKC-UHFFFAOYSA-N

Biochem/physiol Actions

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 μM, 20 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).
Phosphonate precursor (prodrug) of the selective aquaporin 4 (AQP4) inhibitor IMD-0354 (AER-270) with in vivo efficacy in rodent models of brain damage.


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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