LP-935509

LP-935509 is an inhibitor of AP2-associated protein kinase 1 (AAK1) and BMP2-inducible kinase (BIKe, IC50s = 3.3 and 14 nM, respectively). It is selective for AAK1 and BIKe over µ- and kappa-opioid, as well as alpha2A- and alpha2C-adrenergic, receptors (IC50s = >30 µM for all), alpha1 and alpha2 subunit-containing GABAA receptors (IC50s = 12 µM for both), and cyclin G-associated kinase (GAK, IC50 = 0.32 µM). LP-935509 (1 µM) reduces phosphorylation of the synaptic vesicle regulator AP2 complex subunit ?u-1 (AP2M1) in SH-SY5Y neuroblastoma cells. It reduces the number of formalin-induced flinches in mice when administered at doses of 10, 30, and 60 mg/kg.Formal Name: 4-[3-(2-methoxy-3-pyridinyl)pyrazolo[1,5-a]pyrimidin-5-yl]-1-piperazinecarboxylic acid, 1-methylethyl ester. CAS Number: 1454555-29-3. Molecular Formula: C20H24N6O3. Formula Weight: 396.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. lambdamax: 268, 308, 321 nm. SMILES: O=C(N1CCN(CC1)C2=NC3=C(C4=C(OC)N=CC=C4)C=NN3C=C2)OC(C)C. InChi Code: InChI=1S/C20H24N6O3/c1-14(2)29-20(27)25-11-9-24(10-12-25)17-6-8-26-18(23-17)16(13-22-26)15-5-4-7-21-19(15)28-3/h4-8,13-14H,9-12H2,1-3H3. InChi Key: GOOYSJIWTIHOGW-UHFFFAOYSA-N.