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AM6545

Chemical Structure : AM6545

CAS No.: 1245626-05-4

AM6545 (AM 6545)

Catalog No.: PC-20077Not For Human Use, Lab Use Only.

AM6545 (AM-6545) is a potent, selective, oral bioavailable and non-brain-penetrant neutral CB1R antagonist with Ki of 3.3 nM, >100-fold selectivity over CB2R.

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

    Biological Activity

    AM6545 (AM-6545) is a potent, selective, oral bioavailable and non-brain-penetrant neutral CB1R antagonist with Ki of 3.3 nM, >100-fold selectivity over CB2R.
    Unlike rimonabant, AM6545 does not reduce GTPγS binding in mouse brain membranes and is therefore a neutral antagonist.
    AM6545 (10 mg/kg/d for 28 days, oral) improved the metabolic profile in mice with diet-induced obesity (DIO).
    AM6545 exhibited therapeutically relevant efficacy in reducing weight and improving hormonal/metabolic abnormalities in animal models of obesity.
    AM6545 (4.0, 8.0 and 16.0 mg/kg, i.p.) significantly reduced food-reinforced operant responding in vivo.

    Physicochemical Properties

    M.Wt 556.46
    Formula C26H23Cl2N5O3S
    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

    5-(4-[4-cyanobut-1-ynyl]phenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1,1-dioxo-thiomorpholino)-1H-pyrazole-3-carboxamide

    References

    1. Tam J, et al. J Clin Invest. 2010 Aug;120(8):2953-66.

    2. Randall PA, et al. Pharmacol Biochem Behav. 2010 Nov;97(1):179-84.

    3. Limebeer CL, et al. Br J Pharmacol. 2010 Sep;161(2):336-49.

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