| Identification | Back Directory | [Name]
1-{1-[6-(biphenyl-4-ylcarbonyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl]piperidin-4-yl}butan-1-one | [CAS]
1332454-07-5 | [Synonyms]
PK-THPP
PKTHPP,PK THPP
PK-THPP >=98% (HPLC)
1-{1-[6-(biphenyl-4-ylcarbonyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl]piperidin-4-yl}butan-1-one
1-[1-[6-[[1,1'-Biphenyl]-4-ylcarbonyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl]-4-piperidinyl]-1-butanone
1-Butanone, 1-[1-[6-([1,1'-biphenyl]-4-ylcarbonyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl]-4-piperidinyl]- | [Molecular Formula]
C29H32N4O2 | [MOL File]
1332454-07-5.mol | [Molecular Weight]
468.59 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
Soluble in DMSO | [form ]
powder | [color ]
white to beige | [Water Solubility ]
H2O: 10mg/mL, clear
DMSO: 2mg/mL, clear (warmed) | [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 | [InChIKey]
CJZGRIRZVHNUSM-UHFFFAOYSA-N | [SMILES]
O=C(CCC)C(CC1)CCN1C2=C3C(CCN(C(C4=CC=C(C5=CC=CC=C5)C=C4)=O)C3)=NC=N2 |
| Hazard Information | Back Directory | [Uses]
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)[1]. PK-THPP increases breathing rate and induces respiratory alkalosis in rats[2]. | [Biochem/physiol Actions]
PK-THPP is a potent antagonist of tandem pore potassium channel subunit TASK-3 (KCNK9, K2P9.1) with an IC50 value of 35 nM for TASK-3 compared to 303 nM for TASK-1 and with >140 fold selectivity over a wider range of potassium channels. PK-THPP was found to act as a respiratory stimulant, stimulating breathing in isoflurane-anesthetized rats. | [storage]
Store at -20°C | [References]
[1] Coburn CA,et al. Discovery of a pharmacologically active antagonist of the two-pore-domain potassium channel K2P9.1 (TASK-3). ChemMedChem. 2012 Jan 2;7(1):123-33. DOI:10.1002/cmdc.201100351
[2] 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 |
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