An inhibitor of K2P9.1/TASK-3
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PK-THPP

Item No. 29473

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
CAS Number
1332454-07-5
Molecular Formula
C29H32N4O2
Formula Weight
468.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
264 nm
SMILES
O=C(N1CCC2=NC=NC(N3CCC(C(CCC)=O)CC3)=C2C1)C(C=C4)=CC=C4C5=CC=CC=C5
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
InChi Key
CJZGRIRZVHNUSM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $50

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    5 mg

    $134

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    10 mg

    $242

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    25 mg

    $543

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    Product Description

    PK-THPP is a brain-penetrant inhibitor of the two-pore domain potassium channel K2P9.1/TASK-3 (IC50 = 0.035 µM).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Coburn, C.A., Luo, Y., Cui, M., et al. Discovery of a pharmacologically active antagonist of the two-pore-domain potassium channel K2P9.1 (TASK-3). ChemMedChem 7(1), 123-133 (2012).