Pirodavir-R77975-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPirodavirCat. No.: HY-13784CAS No.: 124436-59-5Synonyms: R77975分式: CHNO分量: 369.46作靶点: Enterovirus作通路: Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 10 mg/mL (27.07 mM; Need

2、ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7067 mL 13.5333 mL 27.0665 mL5 mM 0.5413 mL 2.7067 mL 5.4133 mL10 mM 0.2707 mL 1.3533 mL 2.7067 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件

3、，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 1 mg/mL (2.71 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 1 mg/mL (2.71 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师

4、www.MedChemESolubility: 1 mg/mL (2.71 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Pirodavir种有效的核糖核酸病毒抑制剂，效作于 A 和 B 型病毒(rhinovirus)。Pirodavir 常有效作于病毒产量减少试验，IC90 为 2.3 nM。IC50 & Target Rhinovirus 1体外研究 Pirodavir is a potent, broad-spectrum picornavirus inhibitor. Pirodavir inhibits 80 of the 100 human r

5、hinovirus(HRV) strains tested at a concentration of 64 ng/mL. In that same study, Pirodavir is also effective ininhibiting 16 enteroviruses, with a mean 80% inhibitory concentration (IC80) of 1,300 ng/mL. Pirodavir inhibitsenterovirus 71 replication with an IC50 of 5,420 nM and an IC90 of 13,350 nM.

6、 Pirodavir inhibits 56rhinovirus laboratory strains and three of the clinical isolates tested. Pirodavir inhibits 59% of the serotypesand isolates with IC50s of 1. Pirodavir concentrations of 16 and 4g/mL reduces cell growth by 66% (s.e.m.0.75) and 28% (s.e.m. 0.25), respectively. Lower concentratio

7、ns (1g/mL) of Pirodavir are not inhibitory forcell growth. The 50% cytotoxic concentration of pirodavir for logarithmic cell growth at 37C is 7g/mL. Underthe conditions of the antiviral assay (confluent HeLa cells at 33C), the 50% cytotoxic concentration is 50g/mL 2.PROTOCOLCell Assay 2 HeLa cells a

8、re seeded at a concentration of approximately 180,000 cells per dish in six-well plates containing4 mL of growth medium. Growth medium consist of Eagles basal medium, supplemented with 5% fetal calfserum, 2% sodium bicarbonate, and 1% glutamine. After 24 h of incubation at 37C in a humidified CO2atm

9、osphere, the growth medium is removed and replaced by the test solutions (fresh growth medium with orwithout various concentrations of the antiviral compounds). To assess the cytotoxicity of the antiviralcompounds (e.g., Pirodavir), the number of living cells are determined present in triplicate cul

10、tures at the timeof Pirodavir addition and every 24 h for 3 days. Following trypsinization, the number of viable cells for eachdrug concentration is counted in triplicate with a Coulter Counter 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科

11、研献 Nanoscale. 2018 Jan 18;10(3):1440-1452.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Barnard DL, et al. In vitro activity of expanded-spectrum pyridazinyl oxime ethers related to pirodavir: novel capsid-binding inhibitors withpotent antipicornavirus activity. Antimicrob Ag

12、ents Chemother. 2004 May;48(5):1766-72.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE2. Andries K, et al. In vitro activity of pirodavir (R 77975), a substituted phenoxy-pyridazinamine with broad-spectrumantipicornaviralactivity. Antimicrob Agents Chemother. 1992 Jan;36(1):100-7.McePdfHeightCaution: Pr