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TPC2-A1-N

Name: TPC2-A1-N
Brand: TargetMol
SKU: T36805
Price: 199 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T36805Cas No. 136186-07-7

TPC2-A1-N is a novel lipophilic, membrane-permeable subtype-selective TPC2 small molecule agonist that activates endogenous TPC2 to moderately increase lysosomal pH in untransfected cells in a time-dependent manner, and can be used to assay the differential function of TPC2 channels in intact cells.

TPC2-A1-N

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Purity: 99.86%

Catalog No. T36805Cas No. 136186-07-7

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$199	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.86%

Appearance:Solid

Color:White

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COA LCMS

Product Introduction

Bioactivity

Description	TPC2-A1-N is a novel lipophilic, membrane-permeable subtype-selective TPC2 small molecule agonist that activates endogenous TPC2 to moderately increase lysosomal pH in untransfected cells in a time-dependent manner, and can be used to assay the differential function of TPC2 channels in intact cells.
Targets&IC50	Ca2+ current response from TPC2:10.5 μM (EC50), Ca2+:10.5 μM (EC50)
In vitro	Two-pore channels (TPC1-3) are ancient members of the voltage-gated ion channel superfamily, expressed throughout the endo-lysosomal system, and regulate the trafficking of various cargoes. TPC2 mediates different physiological and potentially pathophysiological effects depending on its activation, with its ion selectivity being agonist-dependent. TPC2 uniquely conducts different ions in response to different activating ligands. TPC2-A1-N (10 μM) reproducibly evokes Ca2+ signals, achieving its plateau faster than TPC2-A1-P, with an EC50 of 7.8 μM in cells stably expressing TPC2L11A/L12A. TPC2-A1-N (10 μM) induces Ca2+ influx through TPC2 in TPC2L11A/L12A-expressing cells but not in TPC2L11A/L12A/L265P-expressing cells. TPC2-A1-N responses can be selectively blocked by Tetrandrine, Raloxifene, and Fluphenazine by removing extracellular Ca2+[1]. In endo-lysosomal patch-clamp experiments, TPC2-A1-N (30 μM) elicits Na+ currents in vacuolin-enlarged endo-lysosomes isolated from HEK293 cells transiently expressing human TPC2 (hTPC2) but not in cells expressing TPC1[1]. Furthermore, TPC2-A1-N (30 μM) induces larger currents in endo-lysosomes from cells expressing the gain-of-function TPC2M484L variant compared to the wild-type isoform, with an EC50 of 0.6 μM for TPC2-A1-N[1].

Chemical Properties

Molecular Weight	401.17
Formula	C₁₇H₉Cl₂F₃N₂O₂
Cas No.	136186-07-7
Smiles	O\C(=C(\C#N)C(=O)Nc1ccc(cc1)C(F)(F)F)c1cc(Cl)cc(Cl)c1

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 200 mg/mL (498.54 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (12.46 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4927 mL	12.4635 mL	24.9271 mL	124.6354 mL
5 mM	0.4985 mL	2.4927 mL	4.9854 mL	24.9271 mL
10 mM	0.2493 mL	1.2464 mL	2.4927 mL	12.4635 mL
20 mM	0.1246 mL	0.6232 mL	1.2464 mL	6.2318 mL
50 mM	0.0499 mL	0.2493 mL	0.4985 mL	2.4927 mL
100 mM	0.0249 mL	0.1246 mL	0.2493 mL	1.2464 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc