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Lemborexant

E-2006, (1R,2S)-2-{[(2,4-dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide)
A Potent Antagonist of Orexin1/2 Receptors
Cat #: L-255
Alternative Name E-2006, (1R,2S)-2-{[(2,4-dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide)
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 410.43
    Purity: >99%
    Effective concentration 10-500 nM
    Structure
    Chemical name (1R,2S)-2-[(2,4-dimethylpyrimidin-5-yl)oxymethyl]-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide
    Molecular formula C22H20F2N4O2
    CAS No.: 1369764-02-2
    PubChem CID 56944144
    Activity Lemborexant is a potent and selective dual orexin receptor antagonist (IC50 of 60nM and 11nM on orexin 1 and 2 receptors, respectively). It is brain penetrant and orally bioavailable, demonstrating anxiolytic-like properties in rodents without affecting cognition and motor function1.
    References-Activity
    1. Beuckmann, C.T. et al. (2017) J. Pharmacol. Exp. Ther. 362, 287.
    Shipping and storage Store at -20°C.
    Solubility Soluble up to 50 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 Lemborexant inhibits human OX1 receptors expressed in CHO-K1 cells.
      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.
    References - Scientific background
    1. Beuckmann, C.T. et al. (2017) J. Pharmacol. Exp. Ther. 362, 287.
    2. Spinazzi, R. et al. (2006) Pharmacol. Rev. 58, 46.
    Scientific background

    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.

    Target OX1, OX2 orexin receptors

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    Last update: 23/08/2020

    Lemborexant (#L-255) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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