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- Boss, C., et al (2014) ChemMedChem. 9, 2486.
- Alomone Labs ACT-462206 inhibits human OX1 receptors expressed in CHO-K1 cells.Dose response curve of the normalized inhibition of hOX1 receptor activity by ACT-462206 (#A-450). Cells were loaded with Fluo-8 dye, incubated with increasing concentrations of ACT-462206, 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 293.4 nM.
ACT-462206 is a potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonist with IC50 values of 60 nM and 11 nM, respectively. It has been subjected to clinical trials for use as a sleep inducer1.
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.
ACT-462206 (#A-450) is a highly pure, synthetic, and biologically active compound.