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Pritelivir mesylate

  Cat. No.:  DC32351   Featured
Chemical Structure
1428333-96-3
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More than 5000 active chemicals with high quality for research!
Field of application
Pritelivir, also known as AIC-316 and BAY 57-1293, is a potent helicase primase inhibitor. BAY 57-1293 inhibits replication of herpes simplex virus (HSV) type 1 and type 2 in the nanomolar range in vitro by abrogating the enzymatic activity of the viral primase-helicase complex. In various rodent models of HSV infection the antiviral activity of BAY 57-1293 in vivo was found to be superior compared to all compounds currently used to treat HSV infections. The compound shows profound antiviral activity in murine and rat lethal challenge models of disseminated herpes, in a murine zosteriform spread model of cutaneous disease, and in a murine ocular herpes model. It is active in parenteral, oral, and topical formulations.
Cas No.: 1428333-96-3
Chemical Name: Pritelivir mesylate
Synonyms: Pritelivir mesylate;Pritelivir (mesylate);UQ8YD6U328;N-methyl-N-(4-methyl-5-sulfamoylthiazol-2-yl)-2-(4-(pyridin-2-yl)phenyl)acetamide mesylate;Pritelivir methanesulfonate;Benzeneacetamide, N-(5-(aminosulfonyl)-4-methyl-2-thiazolyl)-N-methyl-4-(2-pyridinyl)-, methanesulfonate (1:1);methanesulfonic acid;N-methyl-N-(4-methyl-5-sulfamoyl-1,3-thiazol-2-yl)-2-(4-pyr;BP180891;methanesulfonic acid;N-methyl-N-(4-methyl-5-sulfamoyl-1,3-thiazol-2-yl)
SMILES: S(C1=C(C)N=C(N(C)C(CC2C=CC(C3C=CC=CN=3)=CC=2)=O)S1)(N)(=O)=O.S(C)(=O)(=O)O
Formula: C19H22N4O6S3
M.Wt: 498.596180438995
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Pritelivir mesylate (BAY 57-1293 mesylate), an inhibitor of the viral helicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV) infection. Pritelivir mesylate is active against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) with the IC50 of 0.02 μM against HSV1-2[1].
Target: IC50: 0.02 μM (HSV1-2)[1]
In Vivo: Pritelivir is the first in a class of antiviral agents that inhibit HSV replication by targeting the viral helicase–primase enzyme complex[2]. Pritelivir (0.03-45 mg/kg) significantly increases survival. Pritelivir (0.3-30 mg/kg) reduces mortality against HSV-1, E-377. Pritelivir has potent and resistance-breaking antiviral efficacy with potential for the treatment of potentially life-threatening HSV type 1 and 2 infections, including herpes simplex encephalitis[3]. Combination therapies of Pritelivir at 0.1 or 0.3 mg/kg/dose with Acyclovir (10 mg/kg/dose) are protective when compared to the vehicle treated group against HSV-2, strain MS[3]. Animal Model: Female BALB/c mice[3] Dosage: 0.03 to 45 mg/kg Administration: Administered orally, twice daily at approximately 12 h intervals, for 7 days Result: Survival was significantly 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%.
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.
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