Pritelivir-BAY-57-1293-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPritelivirCat. No.: HY-15303CAS No.: 348086-71-5Synonyms: BAY 57-1293; AIC316分式: CHNOS分量: 402.49作靶點(diǎn): HSV作通路: Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 33 mg/mL (81.99 mM

2、)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.4845 mL 12.4227 mL 24.8453 mL5 mM 0.4969 mL 2.4845 mL 4.9691 mL10 mM 0.2485 mL 1.2423 mL 2.4845 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Pritelivir (BAY 57-1293; AIC316) 作于HSV he

3、licase primase復(fù)合物，IC50為20 nM。IC50 & Target IC50: 20 nM (HSV-1) 1體外研究BAY 57-1293 is nearly two orders of magnitude more potent than acyclovirin vitro and the superiority was1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEeven more prominent when the viral load was increased (BAY 57-1293 IC50 = 12 nM

4、, 20 nM and 50 nM;acyclovir IC50 = 1uM, 3M and 10 50 uM at a multiplicity of infection (m.o.i.) of 0.0025, 0.02 and 0.2,respectively). A minor increase in IC50 values at higher viral loads was observed for all thiazolyl compoundslisted in Table 1. BAY 57-1293 was also active against porcine (IC50 =

5、5 uM) and bovine (IC50 = 0.12 uM)herpes strains 1.體內(nèi)研究 Delayed treatment with BAY 57-1293 (20 mg/kg 2 daily per os, treatment day 4-14) abrogates progressionof disease symptoms (mean of 10 animals per group) of HSV-2 infected guinea pigs within 1 d of treatmentand healing is observed subsequently, w

6、hereas a 7.5 fold higher dose of valacyclovir (150 mg/kg 2 daily)shows marginal therapeutic efficacy compared with placebo 1. The compound given orally, orintraperitoneally once per day at a dose of 15 mg/kg for 4 successive days was equally effective or superiorto a much higher dose of famciclovir

7、(1mg/ml, i.e. approximately 140-200mg/kg/day) given in the drinkingwater for 7 consecutive days, which, in our hands, is the most effective method for administering famciclovirto mice 2.REFERENCES1. Kleymann G, et al. New helicase-primase inhibitors as drug candidates for the treatment of herpes sim

8、plex disease. Nat Med. 2002Apr;8(4):392-8.2. Biswas S, et al. The helicase primase inhibitor, BAY 57-1293 shows potent therapeutic antiviral activity superior to famciclovir in BALB/cmice infected with herpes simplex virus type 1. Antiviral Res. 2007 Jul;75(1):30-5.McePdfHeightCaution: Product has not been fully validated for medical applications.F