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    Pritelivir (BAY 57-1293)
    Pritelivir (BAY 57-1293)

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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 #: V1747
    CAS #: 348086-71-5Purity ≥98%

    Description: Pritelivir (formerly known as AIC-316; BAY-57-1293; AIC316; BAY571293) is a novel and potent helicase primase inhibitor that displays antiviral effects against herpes simplex virus (HSV) with an IC50 of 20 nM for both HSV-1 and HSV-2. It represents a new class of potent inhibitors of HSV that target the virus helicase primase complex. BAY 57-1293 exhibits anti-herpes activity through inhibiting the helicase-primase and affecting the viral DNA synthesis. In the in vitro viral replication assay, BAY 57-1293 shows inhibition against HSV-1 F, HSV-2 G and acyclovir-resistant HSV-1 F mutant with IC50 value of 20nM. Thus, BAY 57-1293 has significant potential for the treatment of HSV disease in humans, including those resistant to current medications. 

    References: Nat Med. 2002 Apr;8(4):392-8; Antimicrob Agents Chemother. 2002 Jun;46(6):1766-72.

    Related CAS#: 1428333-96-3 (mseylate); 348086-71-5 (free base); 910864-57-2 (HCl); 910864-61-8 (besylate); 2088209-68-9 (sulfate)  

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    Molecular Weight (MW)402.49 
    FormulaC18H18N4O3S2 
    CAS No.348086-71-5 (free base)
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 80 mg/mL (198.8 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILES CodeO=C(N(C)C1=NC(C)=C(S(=O)(N)=O)S1)CC2=CC=C(C3=NC=CC=C3)C=C2
    SynonymsAIC 316; BAY57-1293; BAY 57-1293; AIC-316; BAY-57-1293; AIC316; BAY571293; BAY 571293; BAY-571293; Pritelivir.


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    In Vitro

    In vitro activity: Pritelivir (formerly known as AIC316, BAY 57-1293) is a novel and potent helicase primase inhibitor that showed antiviral effect on herpes simplex virus (HSV) with IC50 of 20 nM for both HSV-1 and HSV-2. It represents a new class of potent inhibitors of HSV that target the virus helicase primase complex. BAY 57-1293 exhibits anti-herpes activity through inhibiting the helicase-primase and affecting the viral DNA synthesis. In the in vitro viral replication assay, BAY 57-1293 shows inhibition against HSV-1 F, HSV-2 G and acyclovir-resistant HSV-1 F mutant with IC50 value of 20nM. Thus, BAY 57-1293 has significant potential for the treatment of HSV disease in humans, including those resistant to current medications. The mechanism of action is that BAY 57-1293 directly inhibits the ATPase activity of the viral helicase-primase enzyme complex in a dose-dependent manner. BAY 57-1293 also shows potent antiviral activity against acyclovir resistant HSV mutants. BAY 57-1293 reduces Aβ and P-tau induced by herpes simplex virus type 1 in vero cells.


    Kinase Assay: Pritelivir (formerly known as AIC316, BAY 57-1293) is a novel and potent helicase primase inhibitor that showed antiviral effect on herpes simplex virus (HSV) with IC50 of 20 nM for both HSV-1 and HSV-2.


    Cell Assay:  In the in vitro viral replication assay, BAY 57-1293 shows inhibition against HSV-1 F, HSV-2 G and acyclovir-resistant HSV-1 F mutant with IC50 value of 20nM. In the plaque reduction assay and the conventional cytopathogenicity assay, BAY 57-1293 shows IC50 values of 0.01-0.02μM and 0.01-0.03μM, respectively. 

    In VivoBAY 57-1293 (p.o.) shows profound antiviral activity in murine and rat lethal challenge models of disseminated herpes (0.5 mg/kg), in a murine zosteriform spread model of cutaneous disease (15 mg/kg), and in a murine ocular herpes model.  
    Animal modelMurine and rat lethal challenge models of disseminated herpes, a murine zosteriform spread model of cutaneous disease, a murine ocular herpes model. 
    Formulation & DosageDissolved in 0.5% tylose in PBS; 0.5 mg/kg or 15 mg/kg; p.o.
    ReferencesNat Med. 2002 Apr;8(4):392-8; Antimicrob Agents Chemother. 2002 Jun;46(6):1766-72; Antiviral Res. 2013 Sep;99(3):401-4.  


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

    Pritelivir (BAY 57-1293)

    Antiviral effect of inhibitors in vitro. Dose-dependent anti-herpes activity of the screening hit BAY 38-9489 (IC50 = 0.5 μM) and development candidate BAY 57-1293 (IC50 = 20 nM) compared with acyclovir (IC50 = 1 μM) determined with the fluorescence-based cytopathogenicity assay.  2002 Apr;8(4):392-8.

     

     Pritelivir (BAY 57-1293)

    Potency and efficacy of compounds in HSV-infected mice. a and b, Superior potency and efficacy of BAY 57-1293 compared with the nucleoside analog valacyclovir (Valtrex) in the murine lethal challenge.  2002 Apr;8(4):392-8.

     


    Pritelivir (BAY 57-1293)

    Compounds inhibit early and late gene expression. 

    Pritelivir (BAY 57-1293)

    Potency and efficacy of compounds in HSV-2-infected guinea pigs. Suppression of acute disease symptoms (photographed at d6 p.i.) of 10 vaginally infected (2.5 × 105 p.f.u. HSV-2 strain MS) female guinea pigs per group.  2002 Apr;8(4):392-8.


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