Powder: -20°C for 3 years | In solvent: -80°C for 1 year
VPS34 inhibitor 1 (Compound 19, PIK-III analogue) (PIK-III analogue) 是一种有效的选择性 VPS34抑制剂( IC50 : 15 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 678 | 现货 | ||
2 mg | ¥ 980 | 现货 | ||
5 mg | ¥ 1,830 | 现货 | ||
10 mg | ¥ 2,990 | 现货 | ||
25 mg | ¥ 5,130 | 现货 | ||
50 mg | ¥ 7,280 | 现货 | ||
100 mg | ¥ 9,790 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,960 | 现货 |
产品描述 | VPS34 inhibitor 1 (Compound 19, PIK-III analogue) (PIK-III analogue) is a potent and selective inhibitor of VPS34( IC50 : 15 nM) |
靶点活性 | VPS34:15 nM |
体外活性 | VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is extraordinarily selective over other lipid and protein kinases. The ability of compound 19 to prevent the degradation of autophagy substrates p62, NCOA4, NBR1, NDP52, and FTH1 is similar to PIK-III. In addition, treatment of cells with compound 19 leads to an increase in the lipidated and nonlipidated forms of LC3 similar to previous reports using PIK-III. |
体内活性 | The pharmacokinetic profile of analogue 19 is determined in C57BL/6 mice.?After oral administration at 10 mg/kg, the compound is rapidly absorbed and showed moderate mean systemic clearance (30 mL/min/kg, approximately 33% of hepatic blood flow), with good oral bioavailability (F% = 47).?Based on these PK parameters and the cellular activity, compound 19 constitutes a suitable candidate for in vivo studies.?Upon oral administration of compound 19 at 50 mg/kg twice a day (BID) for 7 days, LC3-II accumulates consistent with reduced autophagic capacity in time-dependent manner.?It inhibits autophagy in vivo. |
细胞实验 | Cell lines: U2OS cells.Concentrations: 0, 1, 5, 10 μM. Incubation Time: 24 h .Method: For inhibitor assay, cells are plated and the following day when cells had reached 90%, are treated with dimethyl sulfoxide (DMSO, vehicle) or the indicated concentration of PIK-III or Compound 19, both dissolved in DMSO. 24 hours later, cells are lysed in RIPA supplemented with 1% SDS and mini-EDTA protease inhibitors, homogenized by passage through a Qiashredder column and the protein is quantified by DC Lowry protein assay. |
动物实验 | Animal Models: C57BL/6 Mice. Formulation: PG (20% v/v). Dosages: 10 mg/kg(p.o.) or 2 mg/kg(I.V.) .Administration: oral administration or I.V. |
别名 | PIK-III analogue |
分子量 | 391.47 |
分子式 | C21H25N7O |
CAS No. | 1383716-46-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 78 mg/mL (199.25 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5545 mL | 12.7724 mL | 25.5447 mL | 63.8619 mL |
5 mM | 0.5109 mL | 2.5545 mL | 5.1089 mL | 12.7724 mL | |
10 mM | 0.2554 mL | 1.2772 mL | 2.5545 mL | 6.3862 mL | |
20 mM | 0.1277 mL | 0.6386 mL | 1.2772 mL | 3.1931 mL | |
50 mM | 0.0511 mL | 0.2554 mL | 0.5109 mL | 1.2772 mL | |
100 mM | 0.0255 mL | 0.1277 mL | 0.2554 mL | 0.6386 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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