中文名称: L-732138  一键复制产品信息
英文名称: L-732138
CAS No: 148451-96-1
分子式: C22H18F6N2O3
分子量: 472.38
L11032 L-732138 ≥98% (普西唐-psaitong)
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℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):