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BF738735 是有效的磷脂酰肌醇 4-激酶 IIIβ 抑制剂,IC50为 5.7 nM。


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BF738735 是有效的磷脂酰肌醇 4-激酶 IIIβ 抑制剂,IC50为 5.7 nM。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 346 | 现货 | |
| 2 mg | ¥ 523 | 现货 | |
| 5 mg | ¥ 990 | 现货 | |
| 10 mg | ¥ 1,730 | 现货 | |
| 25 mg | ¥ 3,890 | 6-8周 | |
| 50 mg | ¥ 5,570 | 6-8周 | |
| 1 mL x 10 mM (in DMSO) | ¥ 1,090 | 现货 |
BF738735 相关产品
| 产品描述 | BF738735 is a selective inhibitor of phosphatidylinositol 4-kinase III beta (PI4KIIIβ, IC50 = 5.7 nM) showing higher activity over α(IC50 = 1.7 μM). BF738735 exhibits a broad spectrum of antiviral activity. |
| 靶点活性 | PI4KIIIβ:5.7 nM, PI4KIIIα:1.7 μM |
| 体外活性 | BF738735 effectively inhibits all viruses tested, with EC50s ranging between 4 and 71 nM. 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 65 μM, resulting in high selectivity indices. 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 71 nM. BF738735 also impairs PI4KIIIα, but only at an ~300-fold-higher concentration (IC50 of 1.7 μM). The activity of BF738735 is analyzed on a set of 150 cellular kinases, including 13 lipid kinases at a concentration of 10 μM. For all kinases, the inhibition is less than 10%, indicating that BF738735 specifically inhibits PI4KIIIβ in vitro. Low concentrations of BF738735 decrease the amount of luciferase to GuaHCl-treated levels, suggesting that the BF738735 blocks viral RNA replication. The EC50 of BF738735 in this assay is 77 nM, which is comparable to the inhibition observed in the multicycle assay for coxsackievirus serotype B3 (CVB3)[1]. |
| 体内活性 | BF738735 is well tolerated by specimens with good plasma levels of the antiviral in circulation. A complete inhibition with 25 mg/kg and some inhibition with 5 mg/kg dose is observed[2]. |
| 分子量 | 426.46 |
| 分子式 | C21H19FN4O3S |
| CAS No. | 1436383-95-7 |
| Smiles | Cc1nc2c(NCc3cccc(c3)S(C)(=O)=O)nccn2c1-c1ccc(O)c(F)c1 |
| 密度 | 1.42 g/cm3 (Predicted) |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 125 mg/mL (293.11 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.38 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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