| 中文名称: | BF738735 | ||||
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| 英文名称: | BF738735 | ||||
| CAS No: | 1436383-95-7 | 分子式: | C21H19FN4O3S | 分子量: | 426.46 |
| CAS No: | 1436383-95-7 | ||||
| 分子式: | C21H19FN4O3S | ||||
| 分子量: | 426.46 | ||||
基本信息
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产品编号： |
B10637 |
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产品名称： |
BF738735 |
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CAS: |
1436383-95-7 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
426.46 |
-20℃ |
1个月 |
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化学名： |
2-fluoro-4-[2-methyl-8-[(3-methylsulfonylphenyl)methylamino]imidazo[1,2-a]pyrazin-3-yl]phenol |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.3449mL |
11.7244mL |
23.4489mL |
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5mM |
0.4690mL |
2.3449mL |
4.6898mL |
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10mM |
0.2345mL |
1.1724mL |
2.3449mL |
生物活性
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产品描述 |
一种磷脂酰肌醇4-激酶IIIβ (PI4KIIIβ)抑制剂，IC50为5.7nM。 |
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靶点 |
PI4KIIIβ 5.7nM (IC50) |
PI4KIIIα 1.7μM (IC50) |
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体外研究 |
BF738735 (Compound 1) strongly inhibits PI4KIIIβactivity in vitro,with an IC50 of 5.7nM.BF738735 also impairs PI4KIIIα,but only at an ~300-fold-higher concentration (IC50 of 1.7μM).In addition,the activity of BF738735 is analyzed on a set of 150 cellular kinases,including 13 lipid kinases at a concentration of 10μM.For all kinases,the inhibition is less than 10%,indicating that BF738735 specifically inhibits PI4KIIIβin vitro.BF738735 exhibits a broad spectrum of antiviral activity,as it inhibits all tested species of enteroviruses and rhinoviruses,with 50% effective concentrations ranging between 4 and 71nM.BF738735 potently inhibits all viruses tested,with EC50s ranging between 4 and 71nM.The cytotoxicity of BF738735,determined in parallel with the EC50 and using the same culture conditions for 3 to 4 days,is low,with CC50 values ranging from 11 to 65μM,resulting in high selectivity indices.Low concentrations of BF738735 reduce the amount of luciferase to GuaHCl-treated levels,suggesting that the BF738735 blocks viral RNA replication.The EC50 of BF738735 in this assay is 77nM,which is comparable to the inhibition observed in the multicycle assay for coxsackievirus serotype B3 (CVB3). |
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体内研究 |
BF738735 is well tolerated by specimens with good plasma levels of the antiviral in circulation and a complete inhibition with 25mg/kg and some inhibition with 5mg/kg dose is observed. |
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推荐实验方法(仅供参考)
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激酶实验： |
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The PI4K in vitro activity assay is performed. Briefly, recombinant PI4KIIIβ or PI4KIIIα and their substrate,phosphatidylinositol (PI)-phosphatidylserine (PS), are diluted in buffer containing Triton X-100.The reaction is started by addition of a mixture of ATP and 0.25μCi of [γ-33P]ATP. After 75 to 90 min of incubation at 30°C, the reaction is terminated by addition of phosphoric acid. The incorporated radioactivity is measured by using a TopCount NXT microplate scintillation counter. Data are converted to the percent inhibition relative to controls. |
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细胞实验: |
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Buffalo green monkey (BGM) kidney cells,HeLa R19 cells, and HeLa Rh cells are grown at 37℃,5% CO2 in minimal essential medium (MEM) supplemented with 10% fetal bovine serum,penicillin,and streptomycin.The assays to determine the 50% effective concentration (EC50) and 50% cytotoxic concentration (CC50) of BF738735 are performed.Briefly,cells are infected with 100 CCID50 for 2h,after which the virus is removed and serial dilutions of BF738735 (0.01,0.033,0.1,0.33,1,3.33,10,33.33 and 100μM) are added.For determination of the CC50,serial dilutions of BF738735 are added to the cells.Following 3 to 4 days of incubation,the medium is replaced with CellTiter 96 AQueous One solution reagent.Optical densities at 490nm are corrected for background absorbance,which is determined from wells that lack cells.The resulting values for untreated cells are set to 100%. |
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动物实验: |
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Mice BF738735 is used to study the bioavailability and antiviral effect in vivo.BF738735 is administrated in mice,1mg/kg intravenously or 5mg/kg orally to treat coxsackievirus serotype B4 (CVB4) induced pancreatitis. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
