PK-THPP

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