中文名称: EMPA
英文名称: EMPA
CAS No: 680590-49-2
分子式: C27H34N4O4S
分子量: 454.54
E70088 EMPA ≥98% (psaitong)
包装规格:
1mg 5mg 10mg in glass bottle
溶解性:
溶于DMSO(50mg/mL超声)
产品描述:

基本信息

产品编号:

E70088

产品名称:

EMPA

CAS:

680590-49-2

 

储存条件

粉末

-20℃

四年

分子式:

C27H34N4O4S

溶于液体

-80℃

6个月

分子量:

454.54

-20℃

1个月

化学名: 

N-Ethyl-2-((N-(6-methoxypyridin-3-yl)-2-methylphenyl)sulfonamido)-N-(pyridin-3-ylmethyl)acetamide

Solubility (25°C):

 

体外:

 

DMSO

 

Ethanol

'mg/mL

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

2.2000mL

11.0001mL

22.0003mL

5mM

0.4400mL

2.2000mL

4.4001mL

10mM

0.2200mL

1.1000mL

2.2000mL

 

生物活性

产品描述

一种高亲和力的,可逆的选择性 orexin OX2 受体拮抗剂。

靶点

OX2 Receptor

 

体外研究

EMPA competitively antagonizes orexin-A-and orexin-B-evoked accumulation of [3H]inositol phosphates (IP) at hOX2 receptors with pA2 values of 8.6 and 8.8 respectively.EMPA displaces the [3H]EMPA binding from cell membranes containing human and rat OX2 receptors, with Ki values of 1.10±0.24nM and 1.45±0.13nM,respectively.EMPA shows an IC50=5.75µM,Ki=2.63µM,and IC50=12.8µM,Ki=5.8µM in the binding assay at human and mouse V1a receptors,respectively.In CHO(dHFr-) cells stably expressing hOX2 receptors,EMPA inhibits orexin-A-or orexin-B-evoked [Ca2+]i response with IC50s of 8.8±1.7nM and 7.9±1.7nM,respectively.

体内研究

EMPA (1-300mg/kg;i.p.) dose-dependently reverses this [Ala11,D-Leu15]orexin-B-induced hyperlocomotion without itself significantly affecting locomotor activity (LMA) in male NMRI mice.EMPA (3-30 mg/kg; i.p.) induces a significant and dose-dependent reduction in the baseline LMA in france and male Wistar rats.EMPA (3-30mg/kg;i.p.) demonstrates a clear dose-dependent inhibition of spontaneous activity as compared with vehicle-treated animals.

Animal Model:

Male NMRI mice (20-30g)

Dosage:

1,3,10,30,100,300mg/kg

Administration:

Injected i.p.at a volume of 10mL/kg

Result:

Dose-dependently reversed this [Ala11,D-Leu15]orexin-B-induced hyperlocomotion without itself significantly affecting LMA.

 

Animal Model:

France and Male Wistar rats (196-237g)

Dosage:

3,10,30mg/kg

Administration:

Injected i.p.at a volume of 5mL/kg

Result:

Induced a significant and dose-dependent reduction in the baseline LMA. Demonstrated a clear dose-dependent inhibition of spontaneous activity as compared with vehicle-treated animals.

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:
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):