SML2737
AER-271
≥98% (HPLC)
同義詞:
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
推薦產品
品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
−20°C
SMILES 字串
FC(F)(F)c1cc(cc(c1)C(F)(F)F)NC(=O)c2c(ccc(c2)Cl)O[P](=O)(O)O
InChI 密鑰
WSHXPHFIHYXZKC-UHFFFAOYSA-N
生化/生理作用
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.
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Michael Nicosia et al.
Scientific reports, 9(1), 7417-7417 (2019-05-17)
Aquaporins (AQPs) are water channels that mediate a variety of biological processes. However, their role in the immune system is poorly understood. We recently reported that AQP4 is expressed by naïve and memory T cells and that AQP4 blockade with
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