Overview
Cat #:
A-450
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.
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
For research purposes only, not for human use
Last Update: 03/01/2024
Specifications
Citations
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