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mGlu5 PAM 4k

Chemical Structure : mGlu5 PAM 4k

CAS No.: 1382782-16-2

mGlu5 PAM 4k

Catalog No.: PC-60697Not For Human Use, Lab Use Only.

mGlu5 PAM 4k is a potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 130 nM.

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    Biological Activity

    mGlu5 PAM 4k is a potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 130 nM.
    mGlu5 PAM 4k displays 50-fold selectivity over mGlu3, and no activity against mGlu1/2/4/6/7/8.
    mGlu5 PAM 4k shows antipsychotic-like activity in vivo and for treatment of schizophrenia.

    Physicochemical Properties

    M.Wt 338.342
    Formula C18H15FN4O2
    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-(5-fluoropyridin-2-yl)-2-(phenoxymethyl)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one

    References

    1. Conde-Ceide S, et al. Bioorg Med Chem Lett. 2016 Jan 15;26(2):429-434.

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