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Purity: ≥98%
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.
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| ln Vivo |
Pritelivir is the first antiviral medication in a class that targets the viral helicase-primase enzyme complex to prevent HSV replication[2]. The dosage of pritelivir (0.03–45 mg/kg) considerably improves survival. In HSV-1, E-377, pritelivir (0.3–30 mg/kg) lowers mortality. Pritelivir possesses strong and antiviral efficacy that breaks resistance, making it a promising treatment for potentially fatal HSV type 1 and 2 infections, such as herpes simplex encephalitis[3]. When compared to the vehicle-treated group, combination therapies using Pritelivir at 0.1 or 0.3 mg/kg/dose and Acyclovir (10 mg/kg/dose) are protective against HSV-2, strain MS[3].
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| Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse[3]
Doses: 0.03 to 45 mg/kg Route of Administration: Administered orally, twice (two times) daily at approximately 12 h intervals, for 7 days Experimental Results: Survival was Dramatically increased to 80-100% as compared to the vehicle treatment. Even the lowest dose of 0.3 mg/kg was effective in increasing survival to 53%. |
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| References |
[1]. Ligat G, et al. Identification of Amino Acids Essential for Viral Replication in the HCMV Helicase-PrimaseComplex. Front Microbiol. 2018 Oct 23;9:2483.
[2]. Wald A, et al. Helicase-primase inhibitor Pritelivir for HSV-2 infection. N Engl J Med. 2014 Jan 16;370(3):201-10. [3]. Quenelle DC, et al. Efficacy of pritelivir and acyclovir in the treatment of herpes simplex virus infections in a mouse model of herpes simplex encephalitis. Antiviral Res. 2018 Jan;149:1-6. |
| Molecular Formula |
C18H18N4O3S2
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| Molecular Weight |
402.49
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| CAS # |
348086-71-5
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| Related CAS # |
Pritelivir mesylate;1428333-96-3;Pritelivir mesylate hydrate;1428321-10-1
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| SMILES |
O=C(N(C)C1=NC(C)=C(S(=O)(N)=O)S1)CC2=CC=C(C3=NC=CC=C3)C=C2
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4845 mL | 12.4227 mL | 24.8453 mL | |
| 5 mM | 0.4969 mL | 2.4845 mL | 4.9691 mL | |
| 10 mM | 0.2485 mL | 1.2423 mL | 2.4845 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Antiviral effect of inhibitorsin 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.Nat Med.2002 Apr;8(4):392-8. |
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 Potency and efficacy of compounds in HSV-infected mice.aandb, Superior potency and efficacy of BAY 57-1293 compared with the nucleoside analog valacyclovir (Valtrex) in the murine lethal challenge.Nat Med.2002 Apr;8(4):392-8. |
Compounds inhibit early and late gene expression.
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 × 105p.f.u. HSV-2 strain MS) female guinea pigs per group.Nat Med.2002 Apr;8(4):392-8. |
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