L-732138 是一种选择性,有效和竞争性神经激肽-1 (NK-1) 受体拮抗剂,IC50为 2.3 nM。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。
生物活性 | L-732138 is a selective, potent and competitiveneurokinin-1 (NK-1) receptorantagonist with anIC50of 2.3 nM. L-732138 has 200-fold more potent in cloned humanNK-1 receptorsthan cloned ratNK-1 receptors, and has >1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action[1][2]. |
IC50& Target[1][2] | |
体外研究 (In Vitro) | L-732138 (0 -100 μM; first doubling time; COLO 858, MEL HO and COLO 679 cells) treatment results in a concentration-dependent cytotoxicity. L-732138 inhibits cell growth with IC50of 44.6 μM for COLO 858 cells, 76.3 μM for MEL HO cells and 64.2 μM for COLO 679 cells. L-732138 blocks substance P (SP) mitogen stimulation[1]. 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 IC50concentration of 43.6% apoptotic cells for the three melanoma cell lines, whereas at IC100concentration of 51.4 % apoptotic cells[1].
Cell Proliferation Assay[1] 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 | Result: | Resulted in a concentration-dependent cytotoxicity. |
|
体内研究 (In Vivo) | L-732138 (10-4-10-2mol/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[3].
Animal Model: | Male Dunkin-Hartley guinea-pigs (350-500 g) injected with lipopolysaccharide (LPS)[3] | Dosage: | 10-4mol/kg , 10-3mol/kg and 10-2mol/kg | Administration: | Intravenous injection; for 15 minutes | Result: | Abolished the vagally-induced plasma leakage in tracheobronchial tissues, and dose-dependently inhibited the LPS enhanced vagally-induced plasma exudation in traceobronchial tissues. |
|
分子量 | |
性状 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
溶解性数据 | In Vitro: DMSO : 250 mg/mL(529.23 mM;Need ultrasonic) 配制储备液 1 mM | 2.1169 mL | 10.5847 mL | 21.1694 mL | 5 mM | 0.4234 mL | 2.1169 mL | 4.2339 mL | 10 mM | 0.2117 mL | 1.0585 mL | 2.1169 mL |
*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。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 6.25 mg/mL (13.23 mM); Clear solution
此方案可获得 ≥ 6.25 mg/mL (13.23 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 6.25 mg/mL (13.23 mM); Clear solution
此方案可获得 ≥ 6.25 mg/mL (13.23 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
|