TPC2-A1-P is a powerful and membrane permeable agonist of two pore channel 2 (TPC2)with anEC₅₀of 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 induceNa²⁺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^[1][2][3].

EC50: 10.5 μM (TPC2)^[2]

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 (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)^[1].
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^[1].

460.28

Solid

C₂₀H₂₁BrF₃NO₃

Room temperature in continental US; may vary elsewhere.

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

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• 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

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