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 : 9.2 mg/mL (19.63 mM; Need ultrasonic and warming; 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.

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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
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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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