Pritelivir (BAY 57-1293)

Catalog No.S7546

Pritelivir (BAY 57-1293) is a potent helicase primase inhibitor, exhibiting antiviral effect on herpes simplex virus (HSV) with IC50 of 20 nM for both HSV-1 and HSV-2.

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Pritelivir (BAY 57-1293) Chemical Structure

Pritelivir (BAY 57-1293) Chemical Structure
Molecular Weight: 402.49

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Product Information

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Product Description

Biological Activity

Description Pritelivir (BAY 57-1293) is a potent helicase primase inhibitor, exhibiting antiviral effect on herpes simplex virus (HSV) with IC50 of 20 nM for both HSV-1 and HSV-2.
Targets helicase primase [1]
In vitro 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. [1] BAY 57-1293 reduces Aβ and P-tau induced by herpes simplex virus type 1 in vero cells. [3]
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. [2]
Features

Protocol(Only for Reference)

Animal Study: [2]

Animal Models Murine and rat lethal challenge models of disseminated herpes, a murine zosteriform spread model of cutaneous disease, a murine ocular herpes model.
Formulation 0.5 mg/kg or 15 mg/kg
Dosages Suspended in 0.5% tylose in PBS
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Kleymann G, et al. Nat Med. 2002, 8(4), 392-398.

[2] Betz UA, et al. Antimicrob Agents Chemother. 2002, 46(6), 1766-1772.

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Chemical Information

Download Pritelivir (BAY 57-1293) SDF
Molecular Weight (MW) 402.49
Formula

C18 H18 N4 O3 S2

CAS No. 348086-71-5
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms AIC316
Solubility (25°C) * In vitro DMSO 80 mg/mL (198.76 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Benzeneacetamide, N-​[5-​(aminosulfonyl)​-​4-​methyl-​2-​thiazolyl]​-​N-​methyl-​4-​(2-​pyridinyl)​-

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