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TPC2-A1-P

Catalog No. T36806
Synonyms: TPC2-A1-P

TPC2-A1-P is a potent, membrane-permeable agonist of the two-pore channel 2 (TPC2), exhibiting an EC50 of 10.5 μM. It exerts its effects by mimicking the physiological actions of PI(3,5)P2, and demonstrates greater efficacy in inducing Na2+ mobilization from TPC2 compared to TPC-A1-N. This compound serves as a valuable tool for probing various functions of TPC2 channels in intact cells[1][2][3].

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TPC2-A1-P Chemical Structure
TPC2-A1-P, CAS N/A
Pack Size Availability Price/USD Quantity
5 mg Inquiry $ 249.00
10 mg Inquiry $ 415.00
25 mg Inquiry $ 789.00
50 mg Inquiry $ 1,280.00
100 mg Inquiry $ 1,950.00
1 mL * 10 mM (in DMSO) Inquiry $ 252.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TPC2-A1-P is a potent, membrane-permeable agonist of the two-pore channel 2 (TPC2), exhibiting an EC50 of 10.5 μM. It exerts its effects by mimicking the physiological actions of PI(3,5)P2, and demonstrates greater efficacy in inducing Na2+ mobilization from TPC2 compared to TPC-A1-N. This compound serves as a valuable tool for probing various functions of TPC2 channels in intact cells[1][2][3].
In vitro 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].
Synonyms TPC2-A1-P
Molecular Weight N/A

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (108.63 mM), Sonication is recommended.

TargetMolReferences and Literature

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.

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Keywords

TPC2-A1-P TPC2 A1 P TPC2A1P TPC-2-A1-P inhibitor inhibit

 

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