1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Calcium Channel
  3. TPC2-A1-N

TPC2-A1-N 

Cat. No.: HY-131614 Purity: 99.90%
Handling Instructions

TPC2-A1-N is a powerful and Ca2+-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 Ca2+ 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.

For research use only. We do not sell to patients.

TPC2-A1-N Chemical Structure

TPC2-A1-N Chemical Structure

CAS No. : 136186-07-7

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5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
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25 mg USD 1350 In-stock
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50 mg USD 2200 In-stock
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100 mg USD 3400 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

TPC2-A1-N is a powerful and Ca2+-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 Ca2+ 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[1][2].

IC50 & Target

EC50: 10.5 μM (Ca2+ current response from TPC2)[1]

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.
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 Ca2+ 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 TPC2L11A/L12A.
TPC2-A1-N (10 μM) evokes Ca2+ influx through the TPC2 pore evokes Ca2+ signals in cells expressing TPC2L11A/L12A but not TPC2L11A/L12A/L265P. Additionally, the responses to TPC2-A1-N can be selectively blocked by the identified TPC2 blockers Tetrandrine (HY-13764, Tet), Raloxifene (HY-13738, Ral), and Fluphenazine (HY-A0081, Flu) by removal of extracellular Ca2+[1].
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[1].
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 (TPC2M484L) compared to the wild-type isoform, and exhibits an EC50 value of 0.6 μM for TPC2-A1-N[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

401.17

Formula

C₁₇H₉Cl₂F₃N₂O₂

CAS No.
SMILES

O=C(NC1=CC=C(C(F)(F)F)C=C1)/C(C#N)=C(C2=CC(Cl)=CC(Cl)=C2)\O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

TPC2-A1-NCalcium ChannelCa2+ channelsCa channelsNAADPnicotinic acidadenine dinucleotide phosphatelysosomalPI(3,5)P2TPC2Two-pore channellipophilicInhibitorinhibitorinhibit

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TPC2-A1-N
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