名称 | L-732138 |
描述 | L-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 2.3 nM) |
细胞实验 | Cell Line:COLO 858, MEL HO and COLO 679 cells. Concentration:0 μM, 20 μM, 40 μM, 60 μM, 80 μM, 100 μM. Incubation Time:First doubling time[1]. |
动物实验 | Animal Model:Male Dunkin-Hartley guinea-pigs (350-500 g) injected with lipopolysaccharide (LPS)[3].Dosage:10-4 mol/kg ,10-3 mol/kg and 10-2 mol/kg. Administration:Intravenous injection; for 15 minutes[2] |
体外活性 | L-732,138 against three human melanoma cell lines (COLO 858, MEL HO, COLO 679).?L-732,138 elicits cell growth inhibition in a concentration dependent manner in the melanoma cells studied.?Moreover, L-732,138 blocks SP mitogen stimulation.?The specific antitumor action of L-732,138 occurred through the NK-1 receptor and melanoma cell death was by apoptosis[1]. |
体内活性 | L-732138?Abolished the vagally-induced plasma leakage in tracheobronchial tissues, and dose-dependently inhibited the LPS enhanced vagally-induced plasma exudation in traceobronchial tissues[2]. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 4.72 mg/mL (10 mM)
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关键字 | cytotoxicity | vagally-induced | NK receptor | Neurokinin Receptor | Inhibitor | ntravenously | lipopolysaccharide | plasma | Tachykinin receptor | stimulation | L 732138 | mitogen | peralgesia | inhibit | L-732138 | Antitumorhy | L732138 | apoptotic |
相关产品 | Lanepitant 2HCl | Rolapitant | Ezlopitant | (R)-CJ 11974 | N-Acetyl-L-tryptophan | Netupitant | Aprepitant | Vofopitant dihydrochloride | Befetupitant | Vofopitant | Fosaprepitant dimeglumine | Maropitant |
相关库 | 经典已知活性库 | 疼痛相关化合物库 | 神经信号分子库 | 膜蛋白靶向化合物库 | 抑制剂库 | NO PAINS 化合物库 | 已知活性化合物库 | GPCR靶点分子库 | 抗癌化合物库 | 抗癌活性化合物库 |