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HTL14242

Chemical Structure : HTL14242

CAS No.: 1644645-32-8

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HTL14242 (HTL0014242)

Catalog No.: PC-49746Not For Human Use, Lab Use Only.

HTL14242 (HTL0014242) a potent, selective mGlu5 negative allosteric modulator (NAM) with pKi of 9.3 and pIC50 of 9.2, shows high selectivity within the metabotropic family of GPCRs.

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

    Biological Activity

    HTL14242 (HTL0014242) a potent, selective mGlu5 negative allosteric modulator (NAM) with pKi of 9.3 and pIC50 of 9.2, shows high selectivity within the metabotropic family of GPCRs.
    HTL14242 displays 10-100 fold lower affinities and potencies than mavoglurant (pKi 8.0, pIC50 8.0) and dipraglurant (pKi 6.9, pIC50 6.9).
    HTL0014242 (oral dose of 3 mg/kg) demonstrated 80% mGlu5 target receptor occupancy and in rats.

    Physicochemical Properties

    M.Wt 310.72
    Formula C16H8ClFN4
    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

    3-chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile

    References

    1. Bennett KA, et al. Adv Pharmacol. 2020;88:35-58.

    2. Bennett KA, et al. J Pharmacol Exp Ther. 2021 Apr;377(1):157-168.

    3. Christopher JA, et al. J Med Chem 58:6653–6664.

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