An orally bioavailable CysLT1 receptor antagonist (IC50 = 4.3-7.2 nM); selective for the CysLT1 receptor over the CysLT2 receptor (IC50 = 3

Pranlukast – 500 mg

Brand:
Cayman
CAS:
103177-37-3
Storage:
-20
UN-No:
Non-Hazardous - /

Pranlukast is an orally bioavailable cysteinyl leukotriene 1 (CysLT1) receptor antagonist (IC50s = 4.3-7.2 nM in radioligand binding assays).{7174} It is selective for the CysLT1 receptor over the CysLT2 receptor (IC50 = 3,620 nM for the human receptor).{8519} Pranlukast inhibits mucus secretion induced by leukotriene D4 (LTD4; Item No. 20310) in isolated guinea pig trachea with an IC50 value of 0.3 µM.{46532} It inhibits TNF-α-induced NF-ĸB p65 nuclear localization in U937 and Jurkat cells when used at concentrations of 10 and 100 µM.{46533} Pranlukast inhibits bronchoconstriction induced by LTC4 (Item No. 20210), LTD4, and LTE4 (Item No. 20410), but not LTB4 (Item No. 20110), in guinea pigs (ID50s = 0.8, 1, 0.7, and >500 µg/kg, respectively).{46534} It reduces cortical infarct volume by 81.6% and decreases neuronal death in the cortex, hippocampus, and striatum in a rat model of ischemia induced by middle cerebral artery occlusion (MCAO) when administered at a dose of 0.03 mg/kg.{46535}  

 

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SKU: 10008319 - 500 mg Category:

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

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