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Lesogaberan

Chemical Structure : Lesogaberan

CAS No.: 344413-67-8

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Lesogaberan (AZD-3355, AZD3355)

Catalog No.: PC-62764Not For Human Use, Lab Use Only.

Lesogaberan (AZD-3355) is a potent, selective, peripherally acting GABAB receptor agonist with Ki of 5 nM and EC50 of 8.6 nM, 274-fold selectivity over GABAA (Ki=1.4 uM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    Lesogaberan (AZD-3355) is a potent, selective, peripherally acting GABAB receptor agonist with Ki of 5 nM and EC50 of 8.6 nM, 274-fold selectivity over GABAA (Ki=1.4 uM).
    Lesogaberan (AZD-3355) potently stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) through a peripheral mode of action in vivo, shows potential for treatment of GERD.

    Physicochemical Properties

    M.Wt 141.082
    Formula C3H9FNO2P
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    ((R)-3-Amino-2-fluoropropyl)phosphinic acid

    References

    1. Lehmann A, et al. J Pharmacol Exp Ther. 2009 Nov;331(2):504-12.

    2. Brändén L, et al. Eur J Pharmacol. 2010 May 25;634(1-3):138-41.

    3. Alstermark C, et al. J Med Chem. 2008 Jul 24;51(14):4315-20.

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