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VA-012

Chemical Structure : VA-012

CAS No.: 885898-58-8

VA-012 (VA012)

Catalog No.: PC-62010Not For Human Use, Lab Use Only.

VA-012 is a potent, selective 5-HT2C receptor positive allosteric modulator (PAM) that exhibits dose-dependent potentiation of 5-HT efficacy with EC50 of 16 nM.

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    Biological Activity

    VA-012 is a potent, selective 5-HT2C receptor positive allosteric modulator (PAM) that exhibits dose-dependent potentiation of 5-HT efficacy with EC50 of 16 nM.
    VA-012 shows no significant off-target activities, and low binding competition with serotonin or other orthosteric ligands.
    VA-012 increases the anorectic effect combined with the SSRI sertraline.
    VA-012 reduces food intake and body weight gain without causing CNS-related malaise.

    Physicochemical Properties

    M.Wt 313.4
    Formula C21H19N3
    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

    1-(Phenylmethyl)-N-3-pyridinyl-1H-indole-3-methanamine

    References

    1. García Cárceles J, et al. J Med Chem. 2017 Nov 8. doi: 10.1021/acs.jmedchem.7b00994.

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