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TPC2-A1-P
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
TPC2-A1-P图片
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
TPC2-A1-P 是一种强大的膜渗透性的双孔通道 2 (TPC2) 激动剂 (EC50=10.5 μM)，它通过模仿 PI(3,5)P2 的生理作用发挥作用。与 TPC2-A1-N 相比，TPC2-A1-P 具有更高的诱导 Na+ 活化的能力，可用于检测完整细胞中 TPC2 通道的不同功能。
分子式C20H21BrF3NO3
分子量460.28
溶解度DMSO : 50 mg/mL (108.63 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

TPC2-A1-P is a powerful and membrane permeable agonist of two pore channel 2 (TPC2) with an EC50 of 10.5 μM. TPC2-A1-P plays its role by mimicking the physiological actions of PI(3,5)P2. TPC2-A1-P also shows higher potency to induce Na2+ mobilisation from TPC2 than TPC-A1-N . TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells[1][2][3].

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[1].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[1].TPC2-A1-P (10 μM) reproducibly evokes Ca2+ signals, and TPC2-A1-P response reachs its plateau slower than TPC2-A1-N . The EC50 in full concentration-effect relationships for the plateau response is 10.5 μM for TPC2-A1-P in a cell line stably expressing TPC2L11A/L12A.TPC2-A1-P (10-30 μM) induces Ca2+ signals in Hela cells expressing TPC2 in the presence but not absence of extracellular Ca2+. However, the responses are smaller and delayed compared to TPC2-A1-N , consistent with the results obtained in cells stably expressing TPC2L11A/L12A. TPC2-A1-P fails to induce Ca2+ signals in cells expressing ’pore-dead’ TPC2L11A/L12A/L265P and also fails to evoke Ca2+ signals in cells expressing human TRPML1 re-routed to the plasma membrane (TRPML1δNC)[1].In endo-lysosomal patch-clamp experiments, TPC2-A1-P (10 μM) evokes currents in endo-lysosomes isolated from cells expressing TPC2 and TPC2M484L, the currents evoked by TPC2-A1-P are significantly larger than those evoked by TPC2-A1-N in both wild-type and gain-of-function variant,and exhibits an EC50 value of 0.6 μM for TPC2-A1-P[1].

[1]. Susanne Gerndt, et al. Agonist-mediated switching of ion selectivity in TPC2 differentially promotes lysosomal function. Elife. 2020 Mar 16;9:e54712. [2]. Gerndt S, et al. Discovery of lipophilic two-pore channel agonists. FEBS J. 2020;287(24):5284-5293. [3]. Xuhui Jin, et al. Targeting Two-Pore Channels: Current Progress and Future Challenges. Trends Pharmacol Sci. 2020 Aug;41(8):582-594.