TPC2-A1-N - CAS:136186-07-7

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TPC2-A1-N

目录号 : KM6405 CAS No. : 136186-07-7 纯度 : 98%

Data Sheet 产品使用指南

TPC2-A1-N 是一种强大的 Ca²⁺-可渗透双孔通道 2 (TPC2) 的激动剂，通过模拟 NAADP 的生理作用发挥作用。TPC2-A1-N 可诱导 TPC2 显著的 Ca²⁺ 响应 (EC₅₀=7.8 μM)，这种响应并可被一些 TPC 阻断剂阻断。TPC2-A1-N 可用于检测完整细胞中 TPC2 通道的不同功能。

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生物活性

TPC2-A1-N is a powerful and Ca-permeable agonist of two pore channel 2 (TPC2), which plays its role by mimicking the physiological actions of NAADP. TPC2-A1-P reproducibly evokes significant Ca responses from TPC2 (EC₅₀=7.8 μM), and the effect can be blocked by several TPC blockers. TPC2-A1-N 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-N (10 μM) reproducibly evokes Ca 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 TPC2.
TPC2-A1-N (10 μM) evokes Ca influx through the TPC2 pore evokes Ca signals in cells expressing TPC2L11A/L12A but not TPC2. Additionally, the responses to TPC2-A1-N can be selectively blocked by the identified TPC2 blockers Tetrandrine (, Tet), Raloxifene (13738, Ral), and Fluphenazine (, Flu) by removal of extracellular Ca.
In endo-lysosomal patch-clamp experiments, TPC2-A1-N (30 μM) elicits currents using Na as the major permeantion, in vacuolin-enlarged endo-lysosomes isolated from isolated from HEK293 cells transiently expressing human TPC2 (hTPC2) but not in cells expressing TPC1.
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 (TPC2) compared to the wild-type isoform, and exhibits an EC₅₀ value of 0.6 μM for TPC2-A1-N.

分子式

C₁₇H₉Cl₂F₃N₂O₂

分子量

401.17

CAS号

136186-07-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 250 mg/mL (623.18 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4927 mL	12.4635 mL	24.9271 mL
5 mM	0.4985 mL	2.4927 mL	4.9854 mL
10 mM	0.2493 mL	1.2464 mL	2.4927 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.18 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.18 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.18 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。