product name Pritelivir (BAY 57-1293)
Description: Pritelivir (also known as AIC316, BAY 57-1293) is a 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. BAY 57-1293 displays 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.
References: Nat Med. 2002 Apr;8(4):392-8; Antimicrob Agents Chemother. 2002 Jun;46(6):1766-72.
402.49
Formula
C18H18N4O3S2
CAS No.
348086-71-5
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
Solubility (In vivo)
Synonyms
AIC316
other peoduct :
| In Vitro |
In vitro activity: 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: 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 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 & Dosage | Dissolved in 0.5% tylose in PBS; 0.5 mg/kg or 15 mg/kg; p.o. |
| References | Nat Med. 2002 Apr;8(4):392-8; Antimicrob Agents Chemother. 2002 Jun;46(6):1766-72; Antiviral Res. 2013 Sep;99(3):401-4. |
