L-732138 - CAS:148451-96-1

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L-732138

目录号 : KM5755 CAS No. : 148451-96-1 纯度 : 98%

Data Sheet 产品使用指南

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。

规格	价格	是否有货
1mg		In-stock
5mg		In-stock
10mg	询价	In-stock
50mg	询价	In-stock

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生物活性

L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC₅₀ of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-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.

体外研究

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 IC₅₀ of 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.
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:	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

L-732138 (10-10 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 (350-500 g) injected with lipopolysaccharide (LPS)
Dosage:	10 mol/kg , 10 mol/kg and 10 mol/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.

分子式

C₂₂H₁₈N₂O₃F₆

分子量

472.38

CAS号

148451-96-1

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

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。