Pranlukast

Pranlukast is an orally bioavailable cysteinyl leukotriene 1 (CysLT1) receptor antagonist (IC50s = 4.3-7.2 nM in radioligand binding assays). It is selective for the CysLT1 receptor over the CysLT2 receptor (IC50 = 3,620 nM for the human receptor). Pranlukast inhibits mucus secretion induced by leukotriene D4 (LTD4, Cay-20310) in isolated guinea pig trachea with an IC50 value of 0.3 µM. It inhibits TNF-alpha-induced NF-?B p65 nuclear localization in U937 and Jurkat cells when used at concentrations of 10 and 100 µM. Pranlukast inhibits bronchoconstriction induced by LTC4 (Cay-20210), LTD4, and LTE4 (Cay-20410), but not LTB4 (Cay-20110), in guinea pigs (ID50s = 0.8, 1, 0.7, and >500 µg/kg, respectively). 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.Formal Name: N-[4-oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)-benzamide. CAS Number: 103177-37-3. Synonyms: ONO-RS-411, ONO-1078. Molecular Formula: C27H23N5O4. Formula Weight: 481.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:8): 5 mg/ml, DMSO: 10 mg/ml. lambdamax: 255, 315 nm. SMILES: O=C(Nc1cccc2c(=O)cc(oc12)c1[nH]nnn1)c1ccc(OCCCCc2ccccc2)cc1. InChi Code: InChI=1S/C27H23N5O4/c33-23-17-24(26-29-31-32-30-26)36-25-21(23)10-6-11-22(25)28-27(34)19-12-14-20(15-13-19)35-16-5-4-9-18-7-2-1-3-8-18/h1-3,6-8,10-15,17H,4-5,9,16H2,(H,28,34)(H,29,30,31,32). InChi Key: NBQKINXMPLXUET-UHFFFAOYSA-N.