Overview
Cat #:
L-255
Alternative Name E-2006, (1R,2S)-2-{[(2,4-dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide)
Lyophilized Powder yes
Source Synthetic
MW: 410.43
Purity: >99%
Effective concentration 10-500 nM
Structure
Chemical name (1R,2S)-2-[(2,4-dimethylpyrimidin-5-yl)oxymethyl]-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide
Molecular formula C22H20F2N4O2
CAS No.: 1369764-02-2
PubChem CID 56944144
Activity Lemborexant is a potent and selective dual orexin receptor antagonist (IC50 of 60nM and 11nM on orexin 1 and 2 receptors, respectively). It is brain penetrant and orally bioavailable, demonstrating anxiolytic-like properties in rodents without affecting cognition and motor function1.
References-Activity
- Beuckmann, C.T. et al. (2017) J. Pharmacol. Exp. Ther. 362, 287.
Shipping and storage Store at -20°C.
Solubility Soluble up to 50 mM in DMSO. Spin down all products before handling.
Storage of solutions Store at -20°C for several months. It is recommended to aliquot stock solutions to avoid repeated thawing and freezing.
Our bioassay
- Alomone Labs Lemborexant inhibits human OX1 receptors expressed in CHO-K1 cells.Dose response curve of the normalized inhibition of hOX1 receptor activity by Lemborexant (#L-255). Cells were loaded with Fluo-8 dye, incubated with increasing concentrations of Lemborexant, and stimulated with 15 nM Orexin-A. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was calculated at 58.7 nM.
Scientific background
Lemberoxant (E2006) is a potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonist. Lemberoxant binds to both orexin receptors and functionally inhibits them in a competitive manner with low nanomolar potency1.
Orexins are highly conserved proteins known to control feeding behavior, sleep-wake rhythm, reward and addiction and energy balance. In addition, several reports show that orexin/receptor pathways are involved in pathological processes of neurological diseases such as narcolepsy, depression, ischemic stroke, drug addiction and Alzheimer’s disease2.
Target OX1, OX2 orexin receptors
Lyophilized Powder
For research purposes only, not for human use
Last Update: 02/01/2024
Specifications
Citations
Citations