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ACT-462206

(2S)-N-(3,5-Dimethylphenyl)-1-[(4-methoxyphenyl)sulfonyl]-2-pyrrolidinecarboxamide
A Potent Antagonist of Orexin1/2 Receptors
Cat #: A-450
Alternative Name (2S)-N-(3,5-Dimethylphenyl)-1-[(4-methoxyphenyl)sulfonyl]-2-pyrrolidinecarboxamide
  • Bioassay Tested
  • 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
    1. Boss, C., et al (2014) ChemMedChem9, 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.
      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
    1. Hoch, M. et al. (2014) J. Clin. Pharmacol. 54, 979.
    2. 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

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    Last update: 23/08/2020

    ACT-462206 (#A-450) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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    Scientific Background

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