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PFK-158

Name: PFK-158
Brand: TargetMol
SKU: T3105
Price: 248 CNY
Availability: InStock
Rating: 5 (10 reviews)

货号 T3105Cas号 1462249-75-7 一键复制产品信息纯度: 99.16%

很棒

PFK158 是一种选择性的PFKFB3抑制剂，IC50值为 137 nM。它可减少癌细胞中葡萄糖的摄取，ATP 的产生，乳酸的释放，并诱导细胞凋亡和自噬。它还可以增强 Colistin 对细菌的抵抗力，具有广泛的抗肿瘤活性。

PFK-158

一键复制产品信息

很棒

纯度: 99.16%

货号 T3105Cas号 1462249-75-7

为众多的药物研发团队赋能，

让新药发现更简单！

规格	价格	库存
1 mg	¥ 248	现货
5 mg	¥ 625	现货
10 mg	¥ 997	现货
25 mg	¥ 1,810	现货
50 mg	¥ 2,830	现货
100 mg	¥ 4,180	现货
200 mg	¥ 5,970	现货
1 mL x 10 mM (in DMSO)	¥ 478	现货

库存状态实时更新，以官网显示为准，现货产品可直接加购物车下单

大包装 & 定制

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TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

凭借在化合物合成方面的丰富经验，我们可以根据您的研究需求为该产品提供快速定制合成服务。

实验操作小课堂

常见问题解答

选择批次:

纯度: 99.16%

颜色: 白色至黄色

资源下载: COA LCMS产品操作手册

产品介绍

PFK-158 AI Summary

PFK-158 demonstrates diverse bioactivities, including antiviral, antibacterial, enzymatic inhibition, and pharmacokinetic properties. Notably, it exhibits antiviral activity against SARS-CoV-2, with an inhibition rate of 1.89% in Caco-2 cells at 10 µM concentration after 48 hours and -0.1% inhibition in VERO-6 cells under similar conditions, as determined through high content imaging. It also inhibits the SARS-CoV-2 3CL-Pro protease by 18.31% at 20 µM, as measured by a FRET-based assay. The compound shows significant antibacterial activity against various strains, including methicillin-sensitive and resistant Staphylococcus, vancomycin-sensitive and resistant Enterococcus species, and ESBL-positive and negative Escherichia coli. It is particularly more effective against methicillin-sensitive strains and exhibits synergistic activity with colistin against carbapenem-resistant E. coli and Enterobacter cloacae isolates. The cytotoxicity against A549 cells is moderate, with an IC50 value of 15000.0 nM. PFK-158 also functions as an inhibitor of the human HDAC6 enzyme, with 36.79% inhibition using a commercial peptide substrate and -2.03% with a custom peptide substrate. Additionally, it inhibits PFKFB3 in unknown origin cells and Jurkat cells with IC50 values of 137.0 nM and 1600.0 nM, respectively. Metabolically, it has a stability of 37.0% in human liver microsomes and a half-life of 10.5 hours in BALB/c mice, with an AUC of 3235.0 ng.hr.mL-1 and a clearance rate of 26.0 mL.min-1.kg-1 at an intravenous dose of 5 mg/kg. The maximum tolerated dose (MTD) toxicity assessment in Sprague-Dawley rats exceeds 40.0 mg/kg..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	PFK-158 is an effective and specific inhibitor PFKFB3.
靶点活性	PFKFB3:137 nM (IC50 )

化学信息

分子量	328.29
分子式	C₁₈H₁₁F₃N₂O
CAS No.	1462249-75-7
Smiles	FC(F)(F)c1ccc2ccc(\C=C\C(=O)c3ccncc3)nc2c1
密度	1.346 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

DMSO: 35.51 mg/mL (108.17 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0461 mL	15.2304 mL	30.4609 mL	152.3044 mL
5 mM	0.6092 mL	3.0461 mL	6.0922 mL	30.4609 mL
10 mM	0.3046 mL	1.5230 mL	3.0461 mL	15.2304 mL
20 mM	0.1523 mL	0.7615 mL	1.5230 mL	7.6152 mL
50 mM	0.0609 mL	0.3046 mL	0.6092 mL	3.0461 mL
100 mM	0.0305 mL	0.1523 mL	0.3046 mL	1.5230 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

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

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 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / 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 100 μL DMSO （母液浓度为 20 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。