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Pritelivir mesylate hydrate (AIC-316; BAY-57-1293; AIC316; BAY571293) is a 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 robust antiviral activity 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 therapy 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 |
C19H24N4O7S3
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|---|---|
| Molecular Weight |
516.61
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| CAS # |
1428321-10-1
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| Related CAS # |
Pritelivir;348086-71-5;Pritelivir mesylate;1428333-96-3
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| SMILES |
C1=NC(C2C=CC(=CC=2)CC(N(C)C2SC(S(N)(=O)=O)=C(N=2)C)=O)=CC=C1.S(=O)(O)(=O)C.O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9357 mL | 9.6785 mL | 19.3570 mL | |
| 5 mM | 0.3871 mL | 1.9357 mL | 3.8714 mL | |
| 10 mM | 0.1936 mL | 0.9678 mL | 1.9357 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.
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