Chemical Structure : EL-0052
CAS No.:
2093287-60-4
EL-0052
(Lorotomidate, 4-Fluoroetomidate)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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262.28
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Formula
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C14H15FN2O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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Ethyl 4-fluoro-1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylate
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References
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.
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