YM-976

YM-976 is a phosphodiesterase 4 (PDE4) inhibitor (IC50 = 2.2 nM for the human peripheral leukocyte enzyme). It is selective for PDE4 over PDE1, -2, -3, and -5 (IC50s = >3 µM for all). YM-976 inhibits LPS-induced TNF-alpha production in human peripheral blood mononuclear cells (PBMCs). In vivo, YM-976 inhibits carrageenan-induced pleural cavity cell infiltration in a rat model of pleurisy (ED30 = 9.1 mg/kg). It inhibits antigen-induced lung eosinophil infiltration in rats, mice, and ferrets (ED50s = 1.7, 5.8, and 1.2 mg/kg, respectively) and does not induce emesis in ferrets when administered at doses up to 10 mg/kg. YM-976 reduces ovalbumin-induced bronchoconstriction, as well as airway plasma leakage, eosinophil infiltration, and hyperreactivity in a guinea pig model of asthma (ED50s = 7.3, 5.7, 1, and 0.52 mg/kg, respectively). It also reduces citric acid-induced cough in guinea pigs.Formal Name: 4-(3-chlorophenyl)-1,7-diethyl-pyrido[2,3-d]pyrimidin-2(1H)-one. CAS Number: 191219-80-4. Molecular Formula: C17H16ClN3O. Formula Weight: 313.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 3mg/mL, DMSO: 5mg/mL, DMSO:PBS (pH 7.2) (1:3): 0.25mg/mL, Ethanol: 2mg/mL. lambdamax: 224, 352 nm. SMILES: CCC1=CC=C2C(N(CC)C(N=C2C3=CC=CC(Cl)=C3)=O)=N1. InChi Code: InChI=1S/C17H16ClN3O/c1-3-13-8-9-14-15(11-6-5-7-12(18)10-11)20-17(22)21(4-2)16(14)19-13/h5-10H,3-4H2,1-2H3. InChi Key: MNHXYNNKDDXKNP-UHFFFAOYSA-N.