A K2P9.1/TASK-3 inhibitor (IC50 = 0.035 µM); selective for K2P9.1/TASK-3 over K2P2.1/TREK1 and Kv1.5 (IC50s = ~5 and >10 µM

PK-THPP – 10 mg

Brand:
Cayman
CAS:
1332454-07-5
Storage:
-20
UN-No:
Non-Hazardous - /

PK-THPP is a brain-penetrant inhibitor of the two-pore domain potassium channel K2P9.1/TASK-3 (IC50 = 0.035 µM).{53780} It is selective for K2P9.1/TASK-3 over K2P2.1/TREK1 and the voltage-gated potassium channel subtype Kv1.5 (IC50s = ~5 and >10 µM, respectively), as well as a panel of more than 100 receptors, ion channels, and enzymes at 10 µM but does inhibit K2P3.1/TASK-1 (IC50 = 0.3 µM). PK-THPP (100 mg/kg, s.c.) increases the time spent awake and decreases the duration of rapid eye movement (REM) and delta sleep in mice.  

 

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SKU: 29473 - 10 mg Category:

Description

A K2P9.1/TASK-3 inhibitor (IC50 = 0.035 µM); selective for K2P9.1/TASK-3 over K2P2.1/TREK1 and Kv1.5 (IC50s = ~5 and >10 µM, respectively), as well as a panel of more than 100 receptors, ion channels, and enzymes at 10 µM but does inhibit K2P3.1/TASK-1 (IC50 = 0.3 µM); increases the time spent awake and decreases the duration of REM and delta sleep in mice at 100 mg/kg

Formal name: 1-[1-[6-([1,1′-biphenyl]-4-ylcarbonyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl]-4-piperidinyl]-1-butanone

Synonyms: 

Molecular weight: 468.6

CAS: 1332454-07-5

Purity: ≥98%

Formulation: A crystalline solid

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