2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. PK-THPP

PK-THPP is a potent and brain-penetrant TWIK-related acid-sensitive K+ ion channel (K2P9.1 or TASK-3) blocker with IC50s of 35 nM and 300 nM for TASK-3 and TASK-1, respectively. PK-THPP shows no or less activity against other K+ channels. PK-THPP is an effective breathing stimulant and can be used for the study of breathing disorders.

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

PK-THPP Chemical Structure

PK-THPP Chemical Structure

CAS No. : 1332454-07-5

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Based on 1 publication(s) in Google Scholar

PK-THPP Related Antibodies

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Description

PK-THPP is a potent and brain-penetrant TWIK-related acid-sensitive K+ ion channel (K2P9.1 or TASK-3) blocker with IC50s of 35 nM and 300 nM for TASK-3 and TASK-1, respectively. PK-THPP shows no or less activity against other K+ channels. PK-THPP is an effective breathing stimulant and can be used for the study of breathing disorders[1][2].

Cellular Effect
Cell Line Type Value Description References
CHO IC50
300 nM
Compound: 2
Inhibition of TASK-1 (unknown origin) expressed in CHO cells by thallium flux assay
Inhibition of TASK-1 (unknown origin) expressed in CHO cells by thallium flux assay
[PMID: 25017033]
HEK293 IC50
0.035 μM
Compound: 42; PK-THPP
Inhibition of human TASK3 expressed in HEK293 cells by Qpatch HT platform based assay
Inhibition of human TASK3 expressed in HEK293 cells by Qpatch HT platform based assay
[PMID: 31260312]
HEK293 IC50
0.3 μM
Compound: 42; PK-THPP
Inhibition of human TASK1 expressed in HEK293 cells by Qpatch HT platform based assay
Inhibition of human TASK1 expressed in HEK293 cells by Qpatch HT platform based assay
[PMID: 31260312]
In Vitro

PK-THPP (compound 23) is inactive against the K2P channels TREK-1 (IC50 >10 000 nM). PK-THPP is weakly active against the voltage-gated Kv1.5 (IC50 ~5 µM), insensitive to hERG at the highest test concentration (>15 µM), and does not inhibit KATP (<10% inhibition at 10 µM). PK-THPP shows no activity being observed against more than 100 different receptors, ion channels and enzymes (10 µM exposure)[1].

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

PK-THPP Related Antibodies
In Vivo

PK-THPP (15-100 mg/kg; s.c. 3-5 days) has the ability to regulate sleep architecture in rodent electroencephalogram (EEG) telemetry models[1].

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

Animal Model: Male C57/BL6 background or TASK-3 mutant mice and male Sprague–Dawley rats implanted with radiotelemetric monitors[1].
Dosage: 15 mg/kg (rat), 50 mg/kg (rat), 100 mg/kg (mice)
Administration: s.c.; daily; for either three (rat) or five (mice) consecutive days
Result: Increased the time spent awake and decreases the duration of rapid eye movement (REM) and delta sleep in mice.
Dose-dependent effects across all sleep stages were marked by more consistent sleep reductions and greater next-day homeostatic rebound of sleep/wake patterns in rat.
Molecular Weight

468.59

Formula

C29H32N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C2=CC=CC=C2)C=C1)N3CC4=C(N5CCC(C(CCC)=O)CC5)N=CN=C4CC3
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 : 25 mg/mL (53.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1341 mL 10.6703 mL 21.3406 mL
5 mM 0.4268 mL 2.1341 mL 4.2681 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 2.5 mg/mL (5.34 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1341 mL 10.6703 mL 21.3406 mL 53.3515 mL
5 mM 0.4268 mL 2.1341 mL 4.2681 mL 10.6703 mL
10 mM 0.2134 mL 1.0670 mL 2.1341 mL 5.3352 mL
15 mM 0.1423 mL 0.7114 mL 1.4227 mL 3.5568 mL
20 mM 0.1067 mL 0.5335 mL 1.0670 mL 2.6676 mL
25 mM 0.0854 mL 0.4268 mL 0.8536 mL 2.1341 mL
30 mM 0.0711 mL 0.3557 mL 0.7114 mL 1.7784 mL
40 mM 0.0534 mL 0.2668 mL 0.5335 mL 1.3338 mL
50 mM 0.0427 mL 0.2134 mL 0.4268 mL 1.0670 mL
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PK-THPP Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PK-THPP1332454-07-5Potassium ChannelKcsAbrain-penetrantTASK-3K2P9.1Inhibitorinhibitorinhibit

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