TPC2-A1-P|西域试剂

TPC2-A1-P,99.77%

产品编号：Bellancom-131615| 分子式：C₂₀H₂₁BrF₃NO₃| 分子量：460.28

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货号	价格	库存与货期
Bellancom-131615	￥3000.00	杭州北京（现货）
Bellancom-131615	￥5000.00	杭州北京（现货）
Bellancom-131615	￥9500.00	杭州北京（现货）
Bellancom-131615	￥15500.00	杭州北京（现货）
Bellancom-131615	￥23500.00	杭州北京（现货）

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TPC2-A1-P

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 (HY-131614) 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。

生物活性

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 (HY-131614). TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells.

体外研究

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-P (10 μM) reproducibly evokes Ca²⁺ signals, and TPC2-A1-P response reachs its plateau slower than TPC2-A1-N (HY-131614). 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 TPC2^L11A/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 (HY-131614), consistent with the results obtained in cells stably expressing TPC2^L11A/L12A. TPC2-A1-P fails to induce Ca²⁺ signals in cells expressing ‘pore-dead’ TPC2^{L11A/L12A/L265P} and also fails to evoke Ca²⁺ signals in cells expressing human TRPML1 re-routed to the plasma membrane (TRPML1^ΔNC).
In endo-lysosomal patch-clamp experiments, TPC2-A1-P (10 μM) evokes currents in endo-lysosomes isolated from cells expressing TPC2 and TPC2^M484L, the currents evoked by TPC2-A1-P are significantly larger than those evoked by TPC2-A1-N (HY-131614) in both wild-type and gain-of-function variant,and exhibits an EC₅₀ value of 0.6 μM for TPC2-A1-P.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (108.63 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1726 mL	10.8630 mL	21.7259 mL
5 mM	0.4345 mL	2.1726 mL	4.3452 mL
10 mM	0.2173 mL	1.0863 mL	2.1726 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.43 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。