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L-732138
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
L-732138图片
CAS NO:148451-96-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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]

NK1

2.3 nM (IC50)

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

472.38

性状

Solid

Formula

C22H18F6N2O3

CAS 号

148451-96-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL(529.23 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1169 mL10.5847 mL21.1694 mL
5 mM0.4234 mL2.1169 mL4.2339 mL
10 mM0.2117 mL1.0585 mL2.1169 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 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。