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TPC2-A1-N

SKU: orb1693428

Description

TPC2-A1-N is a cell-permeable, subtype-selective agonist for endogenous two-pore channel 2 (TPC2). It facilitates the study of TPC2 function in intact cells by inducing a time-dependent, moderate alkalinization of lysosomal pH. This tool is applicable for lysosomal physiology and channel pharmacology research in both in vitro and in vivo models.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Images & Validation

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TPC2-A1-N

Key Properties

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CAS Number136186-07-7
MW401.17
Purity99.86% (May vary between batches)
FormulaC17H9Cl2F3N2O2
SMILESO\C(=C(\C#N)C(=O)Nc1ccc(cc1)C(F)(F)F)c1cc(Cl)cc(Cl)c1
TargetCalcium Channel
SolubilityDMSO:200 mg/mL (498.54 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (12.46 mM)

Bioactivity

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Target 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+. 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. 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.

Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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TPC2 A1 N, TPC2A1N, TPC-2-A1-N, TPC2-A1-N, TPC2, CalciumChannel, Calcium Channel
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Quick Database Links

Gene Symbol
Calcium Channel

Protocol Information

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1 mg
$ 240.00
DispatchUsually dispatched within 5-10 working days
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