Overview
Alternative Name (2S)-N-(3,5-Dimethylphenyl)-1-[(4-methoxyphenyl)sulfonyl]-2-pyrrolidinecarboxamide
Source Synthetic
MW: 388.48
Purity: >98%
Effective concentration 100 nM - 5 µM
Structure
Chemical name (2S)-N-(3,5-dimethylphenyl)-1-(4-methoxyphenyl)sulfonylpyrrolidine-2-carboxamide
Molecular formula C20H24N2O4S
CAS No.: 1361321-96-1
PubChem CID 40924317
Activity ACT-462206 is a potent and selective dual orexin receptor antagonist (IC50 of 60 nM and 11 nM on orexin 1 and 2 receptors, respectively). ACT-462206 is brain penetrant and orally bioavailable, demonstrating anxiolytic-like properties in rodents without affecting cognition and motor function1.
References-Activity
- Boss, C., et al (2014) ChemMedChem. 9, 2486.
Shipping and storage Store at -20°C.
Solubility Soluble up to 100 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 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.
References - Scientific background
- Hoch, M. et al. (2014) J. Clin. Pharmacol. 54, 979.
- Spinazzi, R. et al. (2006) Pharmacol. Rev. 58, 46.
Scientific background
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.
Target OX1, OX2 orexin receptors
ACT-462206 (#A-450) is a highly pure, synthetic, and biologically active compound.
For research purposes only, not for human use
Last Update: 07/05/2024
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