An inhibitor of PDE4 (IC50s = 54

Ibudilast – 50 mg

Brand:
Cayman
CAS:
50847-11-5
Storage:
-20
UN-No:
Non-Hazardous - /

Ibudilast is an inhibitor of phosphodiesterase 4 (PDE4; IC50s = 54, 65, 239, and 166 nM for PDE4A-D, respectively).{23596} 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-α and fMLP-induced production of leukotriene B4 (LTB4; Item No. 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.{47641} Ibudilast prevents increases in TNF-α, IL-1β, and IL-6 expression in the striatum in a mouse model of MPTP-induced Parkinson’s disease.{47642} 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.  

 

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An inhibitor of PDE4 (IC50s = 54, 65, 239, and 166 nM for PDE4A-D, respectively); selective for PDE4 over PDE1, PDE7A, PDE7B, and PDE9A (IC50 = ≥10,000 nM for all) but does inhibit PDE3A, PDE3B, and PDE5A (IC50s = 1,600, 2,700, and 3,510 nM, respectively); inhibits LPS-induced production of TNF-α and fMLP-induced production of LTB4 in isolated human whole blood (IC50s = 6.2 and 2.5 μM, respectively); inhibits bronchospasm by 34% in a guinea pig model of leukotriene-mediated allergic bronchospasm at 5 mg/kg; prevents increases in TNF-α, IL-1β, and IL-6 expression in the striatum in a mouse model of MPTP-induced Parkinson’s disease; increases striatal expression of GDNF in MPTP-treated and -untreated mice when at 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

Synonyms:  AV 411|KC-404

Molecular weight: 230.3

CAS: 50847-11-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Cell Biology|Cell Signaling|cAMP Signaling||Research Area|Cell Biology|Cell Signaling|cGMP Signaling||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Leukotrienes||Research Area|Immunology & Inflammation|Pulmonary Diseases|Asthma||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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