PK-THPP | CAS#1332454-07-5 | TASK-3 channel blocker

MedKoo Cat#: 562409 | Name: PK-THPP

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PK-THPP is a TASK-3 channel blocker.

Chemical Structure

PK-THPP

CAS#1332454-07-5

Theoretical Analysis

MedKoo Cat#: 562409

Name: PK-THPP

CAS#: 1332454-07-5

Chemical Formula: C29H32N4O2

Exact Mass: 468.2525

Molecular Weight: 468.60

Elemental Analysis: C, 74.33; H, 6.88; N, 11.96; O, 6.83

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 450.00
25mg	USD 950.00

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Related CAS #

No Data

Synonym

PK-THPP; PK THPP; PKTHPP;

IUPAC/Chemical Name

1-{1-[6-(Biphenyl-4-carbonyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl]-piperidin-4-yl}-butan-1-one

InChi Key

CJZGRIRZVHNUSM-UHFFFAOYSA-N

InChi Code

InChI=1S/C29H32N4O2/c1-2-6-27(34)23-13-16-32(17-14-23)28-25-19-33(18-15-26(25)30-20-31-28)29(35)24-11-9-22(10-12-24)21-7-4-3-5-8-21/h3-5,7-12,20,23H,2,6,13-19H2,1H3

SMILES Code

CCCC(C1CCN(C2=C(CN(C(C3=CC=C(C4=CC=CC=C4)C=C3)=O)CC5)C5=NC=N2)CC1)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

PK-THPP is a potent TWIK-related acid-sensitive K(+) ion channel (TASK-3 ion channel) blocker (IC50s are 35 nM and 300 nM for TASK-3 and TASK-1, respectively).

In vitro activity:

TBD

In vivo activity:

TBD

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	23.4	50.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 468.60 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
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

TBD

In vitro protocol:

TBD

In vivo protocol:

TBD

1: Kim D, Hogan JO, White C. TASK inhibition by mild acidosis increases Ca2+ oscillations to mediate pH sensing in rat carotid body chemoreceptor cells. Am J Physiol Lung Cell Mol Physiol. 2023 Mar 1;324(3):L259-L270. doi: 10.1152/ajplung.00099.2022. Epub 2023 Jan 24. PMID: 36692168; PMCID: PMC9970648. 2: Cooper RL, Krall RM. Hyperpolarization Induced by Lipopolysaccharides but Not by Chloroform Is Inhibited by Doxapram, an Inhibitor of Two-P-Domain K+ Channel (K2P). Int J Mol Sci. 2022 Dec 13;23(24):15787. doi: 10.3390/ijms232415787. PMID: 36555429; PMCID: PMC9779748. 3: Konakov MV, Teplov IY, Levin SG, Nenov MN. Anti-hypoxic effect of interleukin-10 in hippocampal neurons is mediated by modulation of TASK-1 and TASK-3 channels activity. Biochem Biophys Res Commun. 2022 Jul 30;615:17-23. doi: 10.1016/j.bbrc.2022.05.051. Epub 2022 May 16. PMID: 35605400. 4: Yang E, Kim W, Park YS, Jin YH. Substance P Increases the Excitability of Dorsal Motor Nucleus of the Vagus Nerve via Inhibition of Potassium Channels. Front Neurosci. 2022 Apr 15;16:867831. doi: 10.3389/fnins.2022.867831. PMID: 35495038; PMCID: PMC9051405. 5: Ramírez D, Mejia-Gutierrez M, Insuasty B, Rinné S, Kiper AK, Platzk M, Müller T, Decher N, Quiroga J, De-la-Torre P, González W. 5-(Indol-2-yl)pyrazolo[3,4-b]pyridines as a New Family of TASK-3 Channel Blockers: A Pharmacophore-Based Regioselective Synthesis. Molecules. 2021 Jun 25;26(13):3897. doi: 10.3390/molecules26133897. PMID: 34202296; PMCID: PMC8271858. 6: García G, Noriega-Navarro R, Martínez-Rojas VA, Gutiérrez-Lara EJ, Oviedo N, Murbartián J. Spinal TASK-1 and TASK-3 modulate inflammatory and neuropathic pain. Eur J Pharmacol. 2019 Nov 5;862:172631. doi: 10.1016/j.ejphar.2019.172631. Epub 2019 Aug 28. PMID: 31472119. 7: Riedelsberger J, Obando PA, Gonzalez W. Yeast strain Saccharomyces cerevisiae BYT45 lacking the cation extrusion systems ENA1-5 and NHA1 is suitable for the characterization of TASK-3 potassium channel antagonists. FEMS Yeast Res. 2019 Aug 1;19(5):foz044. doi: 10.1093/femsyr/foz044. PMID: 31247642. 8: Ramírez D, Bedoya M, Kiper AK, Rinné S, Morales-Navarro S, Hernández- Rodríguez EW, Sepúlveda FV, Decher N, González W. Structure/Activity Analysis of TASK-3 Channel Antagonists Based on a 5,6,7,8 tetrahydropyrido[4,3-d]pyrimidine. Int J Mol Sci. 2019 May 7;20(9):2252. doi: 10.3390/ijms20092252. PMID: 31067753; PMCID: PMC6539479. 9: O'Donohoe PB, Huskens N, Turner PJ, Pandit JJ, Buckler KJ. A1899, PK-THPP, ML365, and Doxapram inhibit endogenous TASK channels and excite calcium signaling in carotid body type-1 cells. Physiol Rep. 2018 Sep;6(19):e13876. doi: 10.14814/phy2.13876. PMID: 30284397; PMCID: PMC6170881. 10: Srisomboon Y, Zaidman NA, Maniak PJ, Deachapunya C, O'Grady SM. P2Y receptor regulation of K2P channels that facilitate K+ secretion by human mammary epithelial cells. Am J Physiol Cell Physiol. 2018 May 1;314(5):C627-C639. doi: 10.1152/ajpcell.00342.2016. Epub 2018 Jan 24. PMID: 29365273; PMCID: PMC6008065. 11: Feng HJ, Faingold CL. Abnormalities of serotonergic neurotransmission in animal models of SUDEP. Epilepsy Behav. 2017 Jun;71(Pt B):174-180. doi: 10.1016/j.yebeh.2015.06.008. Epub 2015 Aug 10. PMID: 26272185; PMCID: PMC4749463. 12: Zeng C, Long X, Cotten JF, Forman SA, Solt K, Faingold CL, Feng HJ. Fluoxetine prevents respiratory arrest without enhancing ventilation in DBA/1 mice. Epilepsy Behav. 2015 Apr;45:1-7. doi: 10.1016/j.yebeh.2015.02.013. Epub 2015 Mar 13. PMID: 25771493; PMCID: PMC4424071. 13: Cotten JF. TASK-1 (KCNK3) and TASK-3 (KCNK9) tandem pore potassium channel antagonists stimulate breathing in isoflurane-anesthetized rats. Anesth Analg. 2013 Apr;116(4):810-6. doi: 10.1213/ANE.0b013e318284469d. Epub 2013 Mar 4. PMID: 23460565; PMCID: PMC3865919.