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Cat #: V1925 CAS #: 1428333-96-3 Purity ≥ 98%
Description: Pritelivir mesylate (formerly known as AIC-316, BAY-571293), the mesylate salt of Pritelivir, is a novel and potent helicase primase inhibitor with antiviral effects against herpes simplex virus (HSV). It inhibits 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.
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
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Molecular Weight (MW) | 498.59 |
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Molecular Formula | C19H22N4O6S3 |
CAS No. | 1428333-96-3 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: > 100 mg/mLr |
Water: N/Ar | |
Ethanol: N/A | |
SMILES Code | O=C(N(C)C1=NC(C)=C(S(=O)(N)=O)S1)CC2=CC=C(C3=NC=CC=C3)C=C2.OS(=O)(C)=O |
Synonyms | AIC 316 mesylate; BAY 57-1293 mesylate; AIC-316 mesylate; BAY-57-1293 mesylate; AIC316 mesylate; BAY57-1293 mesylate; BAY571293 mesylate; BAY 571293 mesylate; BAY-571293 mesylate; Pritelivir mesylate |
Protocol | 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. |
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In Vivo | BAY 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 model | Murine and rat lethal challenge models of disseminated herpes, a murine zosteriform spread model of cutaneous disease, a murine ocular herpes model. | |
Formulation | Dissolved in 0.5% tylose in PBS | |
Dosages | 0.5 mg/kg or 15 mg/kg; p.o. |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.0057 mL | 10.0283 mL | 20.0566 mL | 40.1131 mL |
5mM | 0.4011 mL | 2.0057 mL | 4.0113 mL | 8.0226 mL |
10mM | 0.2006 mL | 1.0028 mL | 2.0057 mL | 4.0113 mL |
20mM | 0.1003 mL | 0.5014 mL | 1.0028 mL | 2.0057 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (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.