Every lot is tried & tested in a relevant biological assay.
- Beuckmann, C.T. et al. (2017) J. Pharmacol. Exp. Ther. 362, 287.
- 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.
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.
Lemborexant (#L-255) is a highly pure, synthetic, and biologically active compound.