Pirodavir-R77975-DataSheet-生命科學(xué)試劑-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作靶點(diǎn): Enterovirus作通路: Anti-infection儲存式: 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 : 10 mg/mL (27.07 mM; Need

2、ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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備液，并請注意儲備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件

3、，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 1 mg/mL (2.71 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 1 mg/mL (2.71 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師

4、www.MedChemESolubility: 1 mg/mL (2.71 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Pirodavir種有效的核糖核酸病毒抑制劑，效作于 A 和 B 型病毒(rhinovirus)。Pirodavir 常有效作于病毒產(chǎn)量減少試驗(yàn)，IC90 為 2.3 nM。IC50 & Target Rhinovirus 1體外研究 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.戶使本產(chǎn)品發(fā)表的科

11、研獻(xiàn) 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 您邊的抑制劑師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