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Pirodavir

Pirodavir

产品编号 T1750   CAS 124436-59-5
别名: R77975, 吡罗达韦

Pirodavir (R77975) 是一种广谱抗小核糖核酸病毒抑制剂,有效抑制人鼻病毒衣壳的结合。

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Pirodavir Chemical Structure
Pirodavir, CAS 124436-59-5
规格 价格/CNY 货期 数量
1 mg ¥ 975 现货
2 mg ¥ 1,430 现货
5 mg ¥ 2,160 现货
10 mg ¥ 2,780 现货
25 mg ¥ 4,690 现货
50 mg ¥ 6,690 现货
100 mg ¥ 8,910 现货
500 mg ¥ 18,200 现货
1 mL * 10 mM (in DMSO) ¥ 1,760 现货
产品目录号及名称: Pirodavir (T1750)
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纯度: 99.78%
纯度: 98.66%
纯度: 98.43%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Pirodavir (R77975) (R 77975), the prototype of broad-spectrum anti-picornavirus compounds, is a potent human rhinovirus (HRV) capsid-binding inhibitor.
体外活性 Pirodavir is a potent, broad-spectrum picornavirus inhibitor. Pirodavir inhibits 80 of the 100 human rhinovirus (HRV) strains tested at a concentration of 64 ng/mL. In that same study, Pirodavir is also effective in inhibiting 16 enteroviruses, with a mean 80% inhibitory concentration (IC80) of 1,300 ng/mL. Pirodavir inhibits enterovirus 71 replication with an IC50 of 5,420 nM and an IC90 of >13,350 nM. Pirodavir inhibits 56 rhinovirus laboratory strains and three of the Clinicalal isolates tested. Pirodavir inhibits 59% of the serotypes and isolates with IC50s of <100 nM[1]. Pirodavir concentrations of 16 and 4μg/mL reduces cell growth by 66% (s.e.m. 0.75) and 28% (s.e.m. 0.25), respectively. Lower concentrations (1μg/mL) of Pirodavir are not inhibitory for cell growth. The 50% cytotoxic concentration of pirodavir for logarithmic cell growth at 37°C is 7μg/mL. Under the conditions of the antiviral assay (confluent HeLa cells at 33°C), the 50% cytotoxic concentration is >50μg/mL[2].
激酶实验 The extract and binding assay buffer consists of 25 mM sodium phosphate, 10 mM potassium fluoride, 10 mM sodium molybdate, 10% glycerol, 1.5 mM EDTA, 2 mM dithiothreitol, 2 mM CHAPS, and 1 mM phenylmethylsulfonyl fluoride (pH 7.4), at room temperature. Intracellular receptors produced in this fashion exhibit reproducible interaction with known ligands at the published affinity. These preparations are subjected to extensive quality control experiments before the assays, covering receptor response, specificity, size, and reference ligand affinity. Receptor assays are performed with a final volume of 250 μL containing from 50-75 μg of extract protein, plus 1-2 nM [3H]Dex at 84 Ci/mmol and varying concentrations of competing ligand (0 to 10 μM). Assays are set up using a 96-well minitube system, and incubations are carried out at 4°C for 18 h. Equilibrium under these conditions of buffer and temperature is achieved by 6-8 h. Nonspecific binding is defined as that binding remaining in the presence of 1000 nM unlabeled Dex. At the end of the incubation period, 200 μL of 6.25% hydroxyapatite are added in wash buffer (binding buffer in the absence of dithiothreitol and phenylmethylsulfonyl fluoride). Specific ligand binding to receptor is determined by a hydroxyapatite-binding assay. Hydroxyapatite absorbs the receptor-ligand complex, allowing for the separation of bound from free radiolabeled ligand. The mixture is vortexed and incubated for 10 min at 4°C and centrifuged, and the supernatant is removed. The hydroxyapatite pellet is washed two times in wash buffer. The amount of receptor-ligand complex is determined by liquid scintillation counting of the hydroxyapatite pellet after the addition of 0.5 mM EcoScint A scintillation cocktail from National Diagnostics[1].
细胞实验 Pirodavir (R 77975) is dissolved in DMSO (10 mg/mL) and stored, and then diluted in growth medium before use[2]. HeLa cells are seeded at a concentration of approximately 180,000 cells per dish in six-well plates containing 4 mL of growth medium. Growth medium consist of Eagle's basal medium, supplemented with 5% fetal calf serum, 2% sodium bicarbonate, and 1% glutamine. After 24 h of incubation at 37°C in a humidified CO2 atmosphere, the growth medium is removed and replaced by the test solutions (fresh growth medium with or without various concentrations of the antiviral compounds). To assess the cytotoxicity of the antiviral compounds (e.g., Pirodavir), the number of living cells are determined present in triplicate cultures at the time of Pirodavir addition and every 24 h for 3 days. Following trypsinization, the number of viable cells for each drug concentration is counted in triplicate with a Coulter Counter[2].
别名 R77975, 吡罗达韦
分子量 369.46
分子式 C21H27N3O3
CAS No. 124436-59-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 11 mg/mL (29.77 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7067 mL 13.5333 mL 27.0665 mL 67.6663 mL
5 mM 0.5413 mL 2.7067 mL 5.4133 mL 13.5333 mL
10 mM 0.2707 mL 1.3533 mL 2.7067 mL 6.7666 mL
20 mM 0.1353 mL 0.6767 mL 1.3533 mL 3.3833 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Barnard DL, et al. In vitro activity of expanded-spectrum pyridazinyl oxime ethers related to pirodavir: novel capsid-binding inhibitors with potent antipicornavirus activity. Antimicrob Agents Chemother. 2004 May;48(5):1766-72. 2. Andries K, et al. In vitro activity of pirodavir (R 77975), a substituted phenoxy-pyridazinamine with broad-spectrum antipicornaviralactivity. Antimicrob Agents Chemother. 1992 Jan;36(1):100-7.
UC-781 Oxamisole TFA Tyrosine kinase-IN-7 Surfen dihydrochloride Paederoside Carrageenan SHEN26 3-Oxobetulin

相关化合物库

该产品包含在如下化合物库中:
ReFRAME 相关化合物库 药物功能重定位化合物库 临床期小分子药物库 已知活性化合物库 免疫/炎症分子化合物库 抗病毒库 抗COVID-19化合物库 非甾体类抗炎化合物库 经典已知活性库 抗感染化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Pirodavir 124436-59-5 Immunology/Inflammation Microbiology/Virology Antiviral Virus Protease Rhinovirus R77975 inhibit R 77975 Enterovirus HEVs HEV Inhibitor HRVs HRV 吡罗达韦 R-77975 inhibitor

 

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