BI-409306

BI-409306 is a potent and selective phosphodiesterase 9A (PDE9A) inhibitor with IC50 values of 65 and 168 nM for the human and rat enzymes, respectively. It is selective for PDE9A over PDE2A, -3A, -4B, -5A, -6AB, -7A and -10A and 95 non-PDE targets at 10 µM but does inhibit human PDE1A and PDE1C (IC50s = 1.45 and 1.17 µM, respectively). BI-409306 (0.5 mg/kg), in combination with MK-801, an NMDA receptor antagonist that reduces cGMP levels, increases cGMP levels by 41% in mouse striatal tissue compared with MK-801 alone. BI 406306 enhances long-term potentiation (LTP) in hippocampal slices and reverses MK-801-induced working memory deficits in a T-maze task in mice when administered at doses ranging from 0.007 to 2.5 mg/kg.Formal Name: 1,5-dihydro-6-(2-pyridinylmethyl)-1-(tetrahydro-2H-pyran-4-yl)-4H-pyrazolo[3,4-d]pyrimidin-4-one. CAS Number: 1189767-28-9. Molecular Formula: C16H17N5O2. Formula Weight: 311.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMF:PBS (pH 7.2) (1:2): 0.33 mg/ml, DMSO: 5 mg/ml. lambdamax: 256 nm. SMILES: O=C(C(C=NN1C2CCOCC2)=C1N3)N=C3CC4=CC=CC=N4. InChi Code: InChI=1S/C16H17N5O2/c22-16-13-10-18-21(12-4-7-23-8-5-12)15(13)19-14(20-16)9-11-3-1-2-6-17-11/h1-3,6,10,12H,4-5,7-9H2,(H,19,20,22). InChi Key: BZTIJCSHNVZMES-UHFFFAOYSA-N.