Description
An orally bioavailable CysLT1 receptor antagonist (IC50 = 4.3-7.2 nM); selective for the CysLT1 receptor over the CysLT2 receptor (IC50 = 3,620 nM for the human receptor); inhibits mucus secretion induced by LTD4 in isolated guinea pig trachea (IC50 = 0.3 µM); inhibits TNF-α-induced NF-ĸB p65 nuclear localization in U937 and Jurkat cells at 10 and 100 µM; inhibits bronchoconstriction induced by LTC4, LTD4, and LTE4, but not LTB4, in guinea pigs (ID50s = 0.8, 1, 0.7, and >500 µg/kg, respectively); reduces cortical infarct volume by 81.6% and decreases neuronal death in the cortex, hippocampus, and striatum in a rat model of MCAO-induced ischemia at 0.03 mg/kg
Formal name: N-[4-oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)-benzamide
Synonyms: ONO-1078|ONO-RS-411
Molecular weight: 481.5
CAS: 103177-37-3
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cell Biology|Cell Signaling|NF-κB Signaling||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Immunology & Inflammation|Pulmonary Diseases|Asthma||Research Area|Lipid Biochemistry|Lipoxygenase Pathways||Research Area|Neuroscience|Neuroprotection|Ischemia