Ibudilast-d7

Ibudilast-d7 is intended for use as an internal standard for the quantification of ibudilast (Cay-14832) by GC- or LC-MS. 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-d3)-1-[2-(1-methylethyl)pyrazolo[1,5-a]pyridin-3-yl]-1-propanone-2,3,3,3-d4. CAS Number: 2713301-45-0. Synonyms: AV 411-d7, KC-404-d7. Molecular Formula: C14H11D7N2O. Formula Weight: 237.4. Purity: >99% deuterated forms (d1-d7). Formulation: (Request formulation change), A solid. Solubility: Chloroform: soluble, Methanol: soluble. SMILES: O=C(C(C([2H])([2H])[2H])([2H])C([2H])([2H])[2H])C(C(C(C)C)=N1)=C2N1C=CC=C2. 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/i3D3,4D3,10D. InChi Key: ZJVFLBOZORBYFE-YDQCIOQBSA-N.