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    JNJ-54175446
    JNJ-54175446

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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 #: V4505
    CAS #: 1627902-21-9Purity ≥98%

    Description: JNJ-54175446 (JNJ54175446) is a novel, potent and selective brain penetrant P2X7 receptor antagonist being developed for treating major depressive disorder. It inhibits hP2X7 receptor and rP2X7 receptor with pIC50s of 8.46 and 8.81, respectively. JNJ-5417544 has suitable physicochemical properties, metabolic stability and an excellent pharmacokinetic profile, good partitioning into the CNS and show robust in vivo target engagement after oral dosing. JNJ-54175446 has been advanced as a candidate to clinical development.  

    References:  2017 Jun 8;60(11):4559-4572


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    JNJ-54175446

    Name: JNJ-54175446
    CAS#: 1627902-21-9
    Chemical Formula: C18H13ClF4N6O
    Exact Mass: 440.0775
    Molecular Weight: 440.7866
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: JNJ54175446; JNJ 54175446; JNJ-54175446
    Chemical Name: (R)-(2-chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyrimidin-2-yl)-4-methyl-1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridin-5-yl)methanone
    InChi Key: CWFVVQFVGMFTBD-SECBINFHSA-N
    InChi Code: InChI=1S/C18H13ClF4N6O/c1-9-15-13(29(27-26-15)17-24-7-10(20)8-25-17)5-6-28(9)16(30)11-3-2-4-12(14(11)19)18(21,22)23/h2-4,7-9H,5-6H2,1H3/t9-/m1/s1
    SMILES Code: ClC1=C(C(F)(F)F)C=CC=C1C(N(CC2)[[email protected]](C)C(N=N3)=C2N3C4=NC=C(C=N4)F)=O


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    Target

    pIC50: 8.46 (hP2X7 receptor), 8.81 (rP2X7 receptor)[1]

    In Vitro JNJ-54175446 (Compound 14) is a potent and selective brain penetrant P2X7 antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 and rP2X7, respectively. JNJ-54175446 shows less potent activity against mouse, dog and Macaque P2X7 (pIC50, 7.8, 7.9 and 8.1, respectively)[1].
    In Vivo JNJ-54175446 shows dose-dependent occupancy with the ED50 of 0.46 mg/kg, corresponding to plasma EC50 of 105 ng/mL[1].
    References

    [1].4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    JNJ-54175446 (JNJ54175446) is a novel, potent and selective brain penetrant P2X7 receptor antagonist being developed for treating major depressive disorder. It inhibits hP2X7 receptor and rP2X7 receptor with pIC50s of 8.46 and 8.81, respectively. 

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