EL-0052 | GABAAR modulator | Probechem Biochemicals

Chemical Structure : EL-0052

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EL-0052 (Lorotomidate, 4-Fluoroetomidate)

货号: PC-25067Not For Human Use, Lab Use Only.

EL-0052 (Lorotomidate, 4-Fluoroetomidate) is a small molecule γ-aminobutyric acid A receptor (GABAAR) modulator, enhances GABAA receptors currents with EC50 of 0.98 uM.

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生物&药学活性

EL-0052 (Lorotomidate, 4-Fluoroetomidate) is a small molecule γ-aminobutyric acid A receptor (GABAAR) modulator, enhances GABAA receptors currents with EC50 of 0.98 uM.
EL-0052 is about three times more potent than etomidate (3.07 ± 1.67 μM).
EL-0052 exhibits loss of righting reflex with ED50s of 1.02 (0.93-1.20) mg/kg in rats and 0.5 (0.45-0.56) mg/kg in dogs.
EL-0052 has a weak inhibition on cortisol biosynthesis in human H259 cells with an IC50 of 1050 nM.
EL-0052 retains the favorable properties of etomidate, including potent hypnotic effect, rapid onset and recovery, stable hemodynamics, and high therapeutic index without suppression of adrenocortical function.

物理化学性质&存储条件

分子量	262.28
分子式	C14H15FN2O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Ethyl 4-fluoro-1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylate

参考文献

1. Jiang JH, et al. Comput Struct Biotechnol J. 2021 Jan 8;19:710-718.

2. Xu X, et al. J Pharmacol Exp Ther. 2021 Dec;379(3):324-330.

3. Patent WO2017059827 A1.

EL-0052 (Lorotomidate, 4-Fluoroetomidate)

生物&药学活性

物理化学性质&存储条件

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EL-0052 (Lorotomidate, 4-Fluoroetomidate)

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物理化学性质&存储条件

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