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Submit ReviewPK-THPP
Description: Potent K2P9.1 (TASK-3) channel blocker
Chemical Name: 1-[1-[6-[[1,1'-Biphenyl]-4-ylcarbonyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl]-4-piperidinyl]-1-butanone
Purity: ≥99% (HPLC)
Biological Activity for PK-THPP
PK-THPP is a potent TASK-3 channel blocker (IC50 = 35 and 300 nM for TASK-3 and TASK-1 respectively). Increases breathing rate and induces respiratory alkalosis in rats.
Compound Libraries for PK-THPP
PK-THPP is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for PK-THPP
| M. Wt | 468.59 |
| Formula | C29H32N4O2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1332454-07-5 |
| PubChem ID | 53464059 |
| InChI Key | CJZGRIRZVHNUSM-UHFFFAOYSA-N |
| Smiles | O=C(C1=CC=C(C2=CC=CC=C2)C=C1)N(C3)CCC4=C3C(N5CCC(C(CCC)=O)CC5)=NC=N4 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PK-THPP
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 23.43 | 50 | |
| 1eq. HCl | 9.37 | 20 with gentle warming |
Preparing Stock Solutions for PK-THPP
The following data is based on the product molecular weight 468.59. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.27 mL | 21.34 mL | 42.68 mL |
| 2.5 mM | 0.85 mL | 4.27 mL | 8.54 mL |
| 5 mM | 0.43 mL | 2.13 mL | 4.27 mL |
| 25 mM | 0.09 mL | 0.43 mL | 0.85 mL |
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Product Datasheets for PK-THPP
References for PK-THPP
References are publications that support the biological activity of the product.
Cotten (2013) TASK-1 (KCNK3) and TASK-3 (KCNK9) tandem pore potassium channel antagonists stimulate breathing in isoflurane-anesthetized rats. Anesth.Analg. 116 810 PMID: 23460565
Coburn et al (2012) Discovery of a pharmacologically active antagonist of the two-pore-domain potassium channel K2P9.1 (TASK-3). ChemMedChem 7 123 PMID: 21916012
If you know of a relevant reference for PK-THPP, please let us know.
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Keywords: PK-THPP, PK-THPP supplier, potent, TASK3, channels, blockers, TWIK, related, acid, sensitive, K+, two, pore, potassium, K2P9.1, subfamily, member, 9, Two-P, Potassium, Channels, 5338, Tocris Bioscience
1 Citation for PK-THPP
Citations are publications that use Tocris products. Selected citations for PK-THPP include:
Veldkamp et al (2018) Neurokinin-3 receptor activation selectively prolongs atrial refractoriness by inhibition of a background K+ channel. Nat Commun 9 4357 PMID: 30341287
Do you know of a great paper that uses PK-THPP from Tocris? Please let us know.
Reviews for PK-THPP
Average Rating: 4 (Based on 1 Review.)
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PH-THPP exhibits concentration dependent blocking activity.
By
Eleanor Baxter on 10/29/2018
Assay Type: In Vitro
Species: Human
A very potent K2p channel blocker which was used to figure out the blocking activity as concentration of the blocker molecule increased. PK-THPP is a great antagonist molecule which shows channel obstructing properties which is concentration dependent.
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