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    JNJ-46778212
    JNJ-46778212

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V4511
    CAS #: 1363281-27-9Purity ≥98%

    Description: JNJ-46778212 (also known as VU 0409551) is a novel, potent, orally bioavailable metabotropic glutamate receptor subtype 5 (mGlu5) positive allosteric modulator (PAMs) with an EC50 of 260 nM. JNJ-46778212 exhibits distinct stimulus bias and selectively potentiates mGlu5 coupling to Gαq-mediated signaling but not mGlu5 modulation of NMDAR currents or NMDAR-dependent synaptic plasticity in the rat hippocampus. On the basis of its robust in vitro potency and in vivo efficacy in multiple preclinical models of multiple domains of schizophrenia, coupled with a good DMPK profile and an acceptable therapeutic window, JNJ-46778212 was selected as a candidate for further development.

    References 2015 May 20;6(6):716-20. 


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    JNJ-46778212

    Name: VU0409551
    CAS#: 1363281-27-9
    Chemical Formula: C20H17FN2O3
    Exact Mass: 352.12232
    Molecular Weight: 352.37
    Elemental Analysis: C, 68.17; H, 4.86; F, 5.39; N, 7.95; O, 13.62
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: JNJ-46778212; JNJ 46778212; JNJ46778212; VU0409551; VU-0409551; VU 0409551;
    IUPAC/Chemical Name: (4-fluorophenyl)(2-(phenoxymethyl)-6,7-dihydrooxazolo[5,4-c]pyridin-5(4H)-yl)methanone
    InChi Key: QUZLMKNNIUSREV-UHFFFAOYSA-N
    InChi Code: InChI=1S/C20H17FN2O3/c21-15-8-6-14(7-9-15)20(24)23-11-10-17-18(12-23)26-19(22-17)13-25-16-4-2-1-3-5-16/h1-9H,10-13H2
    SMILES Code: O=C(N1CCC2=C(OC(COC3=CC=CC=C3)=N2)C1)C4=CC=C(F)C=C4


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    JNJ-46778212


    Chemical evolution of a series of (2(phenoxymethyl)-6,7-dihydrooxazolo[5,4-c]pyridine-5(4H)-yl(aryl)methanones 17 that provided the first mGlu5 PAM clinical candidate.  2015 May 20;6(6):716-20.

     JNJ-46778212


    Molecular pharmacological profile of 17a. (A) Enhanced calcium release induced by suboptimal concentrations of glutamate (EC20), the PAM CRC, with an EC50 for potentiation of 260 nM. (B) Analogue 17a induces a 10-fold leftward shift of the glutamate CRC. (C) Binding study with [3H]-mPEPy, confirming an MPEP sight PAM (Human IC50 = 4.37 μM, 82%). (D) mGlu selectivity data (fold-shift at 10 μM) showing that 17a is highly selective for mGlu5. Each data point represents the mean ± SD (n = 3).

     JNJ-46778212


    Analogue 17a has antipsychotic-like activity in rats and dose-dependently (3–56.6 mg/kg, po) reverses AHL. #,*,∧p < 0.05 vs VAMP group, Dunnett’s test.  2015 May 20;6(6):716-20.


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