Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TPC2-A1-N is a novel, lipophilic, membrane permeable isoform-selective small molecule agonist of two-pore channel 2 (TPC2). TPC2-A1-N plays its role by mimicking the physiological actions of NAADP and PI(3,5)P2 through independent binding sites. TPC2-A1-N has inverse effects on key lysosomal activities and increases the pH in the lysosomal lumen in a TPC2-dependent manner[1].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 3,320 | 5日内发货 | ||
10 mg | ¥ 6,160 | 5日内发货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,840 | 5日内发货 |
产品描述 | TPC2-A1-N is a novel, lipophilic, membrane permeable isoform-selective small molecule agonist of two-pore channel 2 (TPC2). TPC2-A1-N plays its role by mimicking the physiological actions of NAADP and PI(3,5)P2 through independent binding sites. TPC2-A1-N has inverse effects on key lysosomal activities and increases the pH in the lysosomal lumen in a TPC2-dependent manner[1]. |
靶点活性 | Ca2+ current response from TPC2:10.5 μM (EC50) |
体外活性 | Two-pore channels (TPC1-3) are ancient members of the voltage-gated ion channel superfamily. TPCs are expressed throughout the endo-lysosomal system and regulates the trafficking of various cargoes.TPC2 can mediate different physiological and possibly pathophysiological effects depending on how it is activated. The ion selectivity of TPC2 is not fixed but rather agonist-dependent. TPC2 is a unique example of an ion channel that conducts different ions in response to different activating ligands.TPC2-A1-N (10 μM) reproducibly evokes Ca2+ signals, and TPC2-A1-N response reachs its plateau faster than TPC2-A1-P. The EC50 in full concentration-effect relationships for the plateau response is 7.8 μM for TPC2-A1-N in a cell line stably expressing TPC2L11A/L12A.TPC2-A1-N (10 μM) evokes Ca2+ influx through the TPC2 pore evokes Ca2+ signals in cells expressing TPC2L11A/L12A but not TPC2L11A/L12A/L265P. Additionally, the responses to TPC2-A1-N can be selectively blocked by the identified TPC2 blockers Tetrandrine , Raloxifene , and Fluphenazine by removal of extracellular Ca2+[1].In endo-lysosomal patch-clamp experiments, TPC2-A1-N (30 μM) elicits currents using Na+ as the major permeant ion, in vacuolin-enlarged endo-lysosomes isolated from isolated from HEK293 cells transiently expressing human TPC2 (hTPC2) but not in cells expressing TPC1[1].In endo-lysosomal patch-clamp experiments, TPC2-A1-N (30 μM) induces larger currents in endo-lysosomes isolated from cells expressing a gain-of-function variant of TPC2 (TPC2M484L) compared to the wild-type isoform, and exhibits an EC50 value of 0.6 μM for TPC2-A1-N[1]. |
别名 | TPC2-A1-N |
分子量 | 401.17 |
分子式 | C17H9Cl2F3N2O2 |
CAS No. | 136186-07-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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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。
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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。
TPC2-A1-N 136186-07-7 TPC2A1N TPC2 A1 N TPC-2-A1-N Inhibitor inhibitor inhibit