中文名称: | EMPA | ||||
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英文名称: | EMPA | ||||
别名: | N-乙基-2-((N-(6-甲氧基吡啶-3-基)-2-甲基苯基)磺胺基)-N-(吡啶-3-基甲基)乙酰胺 N-Ethyl-2-((N-(6-methoxypyridin-3-yl)-2-methylphenyl)sulfonamido)-N-(pyridin-3-ylmethyl)acetamide | ||||
CAS No: | 680590-49-2 | 分子式: | C27H34N4O4S | 分子量: | 454.54 |
CAS No: | 680590-49-2 | ||||
分子式: | C27H34N4O4S | ||||
分子量: | 454.54 |
基本信息
产品编号: |
E70088 |
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产品名称: |
EMPA |
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CAS: |
680590-49-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
454.54 |
-20℃ |
1个月 |
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化学名: |
N-Ethyl-2-((N-(6-methoxypyridin-3-yl)-2-methylphenyl)sulfonamido)-N-(pyridin-3-ylmethyl)acetamide |
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Solubility (25°C): |
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体外:
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DMSO |
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Ethanol |
'mg/mL |
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Water |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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靶点 |
OX2 Receptor |
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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. |
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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. |
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Animal Model: |
Male NMRI mice (20-30g) |
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Dosage: |
1,3,10,30,100,300mg/kg |
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Administration: |
Injected i.p.at a volume of 10mL/kg |
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Result: |
Dose-dependently reversed this [Ala11,D-Leu15]orexin-B-induced hyperlocomotion without itself significantly affecting LMA. |
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Animal Model: |
France and Male Wistar rats (196-237g) |
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Dosage: |
3,10,30mg/kg |
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Administration: |
Injected i.p.at a volume of 5mL/kg |
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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. |
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
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 )