Ibudilast

Ibudilast is an inhibitor of phosphodiesterase 4 (PDE4, IC50s = 54, 65, 239, and 166 nM for PDE4A-D, respectively). It is selective for PDE4 over PDE1, PDE7A, PDE7B, and PDE9A (IC50s = >10,000 nM for all) but does inhibit PDE3A, PDE3B, and PDE5A (IC50s = 1,600, 2,700, and 3,510 nM, respectively). Ibudilast inhibits LPS-induced production of TNF-alpha and fMLP-induced production of leukotriene B4 (LTB4, Cay-20110) in isolated human whole blood (IC50s = 6.2 and 2.5 µM, respectively). It inhibits bronchospasm by 34% in a guinea pig model of leukotriene-mediated allergic bronchospasm when administered intravenously at a dose of 5 mg/kg. Ibudilast prevents increases in TNF-alpha, IL-1beta, and IL-6 expression in the striatum in a mouse model of MPTP-induced Parkinson's disease. It also increases striatal expression of glial cell-derived neurotrophic factor (GDNF) in MPTP-treated and -untreated mice when administered at doses of 40 and 50 mg/kg, respectively, twice per day.Formal Name: 2-methyl-1-[2-(1-methylethyl)pyrazolo[1,5-a]pyridin-3-yl]-1-propanone. CAS Number: 50847-11-5. Synonyms: AV 411, KC-404. Molecular Formula: C14H18N2O. Formula Weight: 230.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 16 mg/ml, Ethanol: 25 mg/ml, Ethanol:PBS (pH 7.2) (1:11): 0.08 mg/ml. lambdamax: 227, 263, 321 nm. SMILES: CC(C)C1=NN(C=CC=C2)C2=C1C(C(C)C)=O. InChi Code: InChI=1S/C14H18N2O/c1-9(2)13-12(14(17)10(3)4)11-7-5-6-8-16(11)15-13/h5-10H,1-4H3. InChi Key: ZJVFLBOZORBYFE-UHFFFAOYSA-N.