中文名称: 盐酸氯吡胺
英文名称: Chloropyramine hydrochloride
CAS No: 6170-42-9
分子式: C16H20ClN3.HCl
分子量: 326.26
EINEC: 228-216-2
C11021 盐酸氯吡胺 ≥98% (psaitong)
包装规格:
100mg in glass bottle
溶解性:
溶于DMSO(30mg/mL超声)
产品描述:

基本信息

产品编号:

C11021 

产品名称:

Chloropyramine hydrochloride

CAS:

6170-42-9

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C16H20ClN3.HCl

溶于液体

-80℃

6个月

分子量:

326.26

-20℃

1个月

化学名: 

N1-(4-Chlorobenzyl)-N2,N2-dimethyl-N1-(pyridin-2-yl)ethane-1,2-diamine hydrochloride

Solubility (25°C):

 

体外:

 

DMSO

65mg/mL (199.22mM)

Ethanol

 

Water

 

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

3.0650mL

15.3252mL

30.6504mL

5mM

0.6130mL

3.0650mL

6.1301mL

10mM

0.3065mL

1.5325mL

3.0650mL

50mM

0.0613mL

0.3065mL

0.6130mL

 

生物活性

产品描述

一种组胺受体 H1 (histamine receptor H1) 拮抗剂,它也能抑制 VEGFR-3 和 FAK 的生化功能。

靶点

VEGFR-3

 

体外研究

BT474 cells are highly sensitive to Chloropyramine hydrochloride (compound 1) treatment,whereby 1µM concentrations cause a 40% reduction of viability after 48h of treatment.It is found that at 1µM concentrations of Chloropyramine hydrochloride,viability of control MCF7-pcDNA3 cells is significantly higher than the viability of MCF7-VEGFR-3 cells (P<0.01) and at 10µM concentration this difference reaches twofold (P<0.001).In the BT474 cells treatment with Chloropyramine hydrochloride also leads to a concentration-dependent decrease of cell proliferation. When treatment with Chloropyramine hydrochloride is continued for 48h,the breast cancer cells that overexpressed VEGFR-3 undergo apoptosis.This effect is dose-dependent,with 10µM Chloropyramine hydrochloride inducing apoptosis in more than 60% of BT474 cells.In our model cell lines MCF7-pcDNA3 and MCF7-VEGFR-3,treatment with 10µM Chloropyramine hydrochloride for 48h leads to a 4-fold increase in apoptotic cell death in the cell line that overexpressed VEGFR-3 (18% versus 76 % respectively).

体内研究

Chloropyramine hydrochloride causes a dramatic reduction of tumor growth in both model systems whereby the tumor size in the treated groups is approximately 20% of the tumor size in vehicle control groups.Doxorubicin administered at 3mg/kg causes approximately 60% reduction of tumor growth,but has no effect on tumor growth at 0,3mg/kg.In contrast, there is a modest effect of Chloropyramine hydrochloride alone (50% reduction of tumor growth).The low-dose combination of Chloropyramine hydrochloride and doxorubicin has a prolonged anti-tumor effect (85% reduction of tumor growth) that is greater than either drug alone.

 

推荐实验方法(仅供参考)

激酶实验:

Cells are incubated in presence or absence of Chloropyramine hydrochloride and stained with anti-FAK antibody 4.47 or in combination with paxillin or VEGFR-3.Detection is done with Alexa Fluor 546 secondary antibody and for dual staining combination of Alexa Fluor 488 and Alexa Fluor 546 secondary antibody is used.

 

细胞实验:

 

Cell survival is assayed in MTS assay by measuring mitochondrial dehydrogenase activity of metabolically active cells.5.0×103 (100 µL) cells are plated in 96-well plates and are allowed to attach overnight. One hundred microliters of fresh media with or without Chloropyramine hydrochloride is added to each well. Cells are treated for designated amount of time. MTS assay is performed according the manufacturers protocol.

 

动物实验:

 

BT474 and MCF7-VEGFR-3 cells at a concentration of 2 to 5×106 cells per 200µL are subcutaneously injected into the right flank of the 5 to 6 week old mice,5 in each group.Treatment with Chloropyramine hydrochloride is started next day after cells injection via intraperitoneal injection (IP) once a day.Tumor size is measured thrice weekly and volume is calculated using the formula length×width2×0.5.Animals are sacrificed after 21 days of treatment or when tumor size reaches protocol end point.Tumor is excised, measured and preserved for protein and RNA preparation and cytochemistry.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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:
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摩尔浓度计算公式

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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    C8=C7/X C8: LOG(C8):