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L-732138  ≥98%

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包装规格：10mg 50mg 100mg 250mg in glass bottle
溶解性：溶于DMSO(250mg/mL超声）
产品描述：基本信息 产品编号： L11032 产品名称： L-732138 CAS: 148451-96-1   储存条件 粉末 -20℃ 四年     分子式： C22H18F6N2O3 溶于液体 -80℃ 6个月 分子量： 472.38 -20℃ 1个月 化学名：  3,5-Bis(trifluoromethyl)benzyl N-acetyltryptophan Solubility (25°C)：   体外:   DMSO 94mg/mL (198.99mM) Ethanol 94mg/mL (198.99mM) Water Insoluble 体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.1169mL 10.5847mL 21.1694mL 5mM 0.4234mL 2.1169mL 4.2339mL 10mM 0.2117mL 1.0585mL 2.1169mL 50mM 0.0423mL 0.2117mL 0.4234mL   生物活性 产品描述 一种选择性，有效和竞争性神经激肽-1 (NK-1) 受体拮抗剂，IC50 为 2.3nM。L-732138 在克隆的人 NK-1 受体中的效力比在克隆大鼠 NK-1 受体中高 200 倍，比人类 NK-2 和 NK-3 受体高 1000 倍以上。L-732138 可减轻痛觉过敏并具有抗肿瘤作用。 靶点 NK-1 receptor(in CHO cells) 2.3nM   体外研究 L-732138 (0-100µM;first doubling time;COLO 858,MEL HO and COLO 679 cells) treatment results in a concentrationdependent cytotoxicity.L-732138 inhibits cell growth with IC50 of 44.6μM for COLO 858 cells, 76.3μM for MEL HO cells and 64.2μM for COLO 679 cells.L-732138 blocks substance P (SP) mitogen stimulation.L-732,138 treatment results in a large number of apoptotic cells were found in COLO 858,MEL HO and COLO 679 melanoma cell lines.In DAPI-stained cultures,at IC50 concentration of 43.6% apoptotic cells for the three melanoma cell lines,whereas at IC100 concentration of 51.4 % apoptotic cells. Cell Proliferation Assay Cell Line: COLO 858,MEL HO and COLO 679 cells Concentration: 0µM,20µM,40µM,60µM,80µM,100µM Incubation Time: First doubling time Result: Resulted in a concentration-dependent cytotoxicity. 体内研究 L-732138 (10-4-10-2 mol/kg;intravenous injection;for 15 minutes;male Dunkin-Hartley guinea-pigs) treatment abolishes vagally-induced plasma exudation and significantly inhibits the enhancement by LPS.The LPS-enhanced vagally-induced plasma exudation is not completely inhibited by either L-732138 or SOD pretreatment alone,but is blocked by the combination of both pretreatments. Animal Model: Male Dunkin-Hartley guinea-pigs (350-500g) injected with lipopolysaccharide (LPS) Dosage: 10-4 mol/kg ,10-3 mol/kg and 10-2 mol/kg Administration: Intravenous injection;for 15 minutes Result: Abolished the vagally-induced plasma leakage in tracheobronchial tissues,and dosedependently inhibited the LPS enhanced vagally-induced plasma exudation in traceobronchial tissues.
保存条件：-20℃

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