Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PF-06649298 是一种钠偶联柠檬酸盐转运蛋白抑制剂,可用于调节糖代谢以及脂代谢的研究。PF-06649298 在人类肝细胞中与 NaCT 特异性结合从而抑制柠檬酸盐的转运,IC50值为 16.2 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 3,730 | 5日内发货 | ||
10 mg | ¥ 6,990 | 5日内发货 | ||
1 mL * 10 mM (in DMSO) | ¥ 4,120 | 5日内发货 |
产品描述 | PF-06649298 is an inhibitor of sodium-coupled citrate transporter which specifically interacts with NaCT with an IC 50 value of 16.2 μM to inhibits the transport of citrate in human hepatocytes. PF-06649298 can be used in regulating metabolism of glucose and metabolism of lipid [1] [2]. |
体外活性 | PF-06649298 (0-100 μM; 30 min) inhibits citrate uptaken in cells [2]. Cell Viability Assay [1] Cell Line: HEK-293 cells expressing NaCT, NaDC1 or NaDC3, human hepatocytes and mouse epatocytes Concentration: 0-100 μM Incubation Time: 30 min Result: Showed a selectivity for NaCT over the dicarboxylate transporters NaDC1 and NaDC3. Inhibited citrate uptake in HEK-293 cells expressing NaCT, NaDC1 or NaDC3, human hepatocytes and mouse epatocytes with IC 50 s of 408 nM, >100 μM, >100 μM, 16.2 μM and 4.5 μM, respectively. |
体内活性 | PF-06649298 (250 mg/kg; p.o. twice a day; for 21 days) reverses glucose intolerance of HFD mice [1]. Animal Model: Mice with HFD administration [2] Dosage: 250 mg/kg Administration: Oral gavage; 250mg/kg twice a day; for 21 days Result: Decreased plasma glucose, hepatic triglycerides, diacylglycerides, and acyl-carnitines concentration of livers in HFD mice. Totally reversed glucose intolerance of HFD mice. |
分子量 | 294.34 |
分子式 | C16H22O5 |
CAS No. | 1854061-16-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
PF-06649298 1854061-16-7 Inhibitor inhibitor inhibit