2. GPCR/G Protein Neuronal Signaling Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation MAPK/ERK Pathway
  3. Opioid Receptor Apoptosis Reactive Oxygen Species (ROS) NO Synthase Toll-like Receptor (TLR) p38 MAPK NF-κB
  4. Nalmefene

Nalmefene 是一种能透过血脑屏障的阿片受体调节剂，是 MOR 和 DOR 拮抗剂，也是 KOR 部分激动剂。Nalmefene 具有抗炎、神经保护的活性。Nalmefene 可用于减少酒精依赖性疾病的研究。

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Nalmefene Chemical Structure

Nalmefene Chemical Structure

CAS No. : 55096-26-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660
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5 mg ￥600
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10 mg ￥900
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25 mg ￥1800
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50 mg ￥2850
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100 mg ￥4500
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200 mg   询价  
500 mg   询价  

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Customer Review

Other Forms of Nalmefene:

Nalmefene 相关抗体

Top Publications Citing Use of Products

查看 Opioid Receptor 亚型特异性产品:

查看所有亚型
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

查看 NO Synthase 亚型特异性产品:

查看所有亚型
nNOS iNOS eNOS

查看 Toll-like Receptor (TLR) 亚型特异性产品:

查看所有亚型
TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Nalmefene is a BBB-penetrable opioid receptor modulator. Nalmefene is an antagonist of MOR and DOR, and a partial agonist of KOR. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders[1][2][3][4].

IC50 & Target

MOR, DOR, KOR[2]
体外研究
(In Vitro)

Nalmefene (0.01-300 μM；1.5-3.5 h) 在原代培养的星形胶质细胞中，可抑制乙醇刺激下 ROS 生成、iNOS 合成，并阻断 TLR4 信号通路以及 MAPKs 磷酸化、NF-κB 激活，减少细胞死亡[1]。
Nalmefene (0-300 μg/mL; 24 h) 在 RAW264.7 细胞，可促进 CD36 表达，并使 μ-、δ- 和 κ- 阿片受体的 mRNA 水平分别降低 73%、56% 和 39%[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Nalmefene 相关抗体:

Western Blot Analysis[1]

Cell Line: Primary cultured astrocytes treated ethanol
Concentration: 0.01, 0.1 and 1 μM
Incubation Time: retreated with 0.5 h, then co-incubation for 1 h
Result: Inhibited the levels of iNOS.

Real Time qPCR[2]

Cell Line: RAW264.7
Concentration: 300 μg/mL
Incubation Time: 24 H
Result: Inhibited the mRNA levels of μ-, δ- and κ-opioid receptors.
体内研究
(In Vivo)

Nalmefene (0.1 mg/kg; 腹腔注射; 四天 2 次; 2 周) 在小鼠中，可预防乙醇诱导的神经炎症、髓鞘损伤和细胞凋亡，以及小鼠的饮酒偏好和摄入量[1]。
Nalmefene (1-3 mg/kg; 皮下注射; 21 天) 在高脂饮食的 ApoE KO 小鼠中加重动脉粥样硬化斑块的形成[2]。
Nalmefene (0.032-1 mg/kg; 腹腔注射; 单剂量) 在小鼠中对吗啡起到拮抗作用[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C57BL/6 treated ethanol[1]
Dosage: 0.1 mg/kg
Administration: Intraperitoneal injection (i.p.); 2 consecutive days, followed by 2-day gaps with no injections for 2 weeks
Result: Significantly inhibited the up-regulation of inflammatory cytokines, chemokines, and pro-inflammatory mediators in the prefrontal cortex (PFC) and striatum/nucleus accumbens (STR/NAcc) induced by ethanol treatment.
Protected against myelin damage and cell death in these brain regions.
abolished the increase in alcohol preference and consumption caused by intermittent ethanol treatment in mice.
Inhibited the up-regulation of transcriptional factors related to ethanol consumption and addictive behavior in the PFC and STR/NAcc.
Animal Model: Male C57BL/6J ApoE knockout mice aged 8 weeks old were fed a high-fat diet[2]
Dosage: 1 and 3 mg/kg
Administration: Subcutaneous injection (s.c.); 21 days
Result: Significantly increased atherosclerotic plaque formation in the whole aorta, aortic arch, and aortic root of the ApoE KO mice in a dose-dependent manner.
Elevated the plasma levels of total cholesterol and triglycerides.
Animal Model: Male ICR mice (25-35 g)[3]
Dosage: Locomotor studies and antinociceptive studies: 0.32 mg/kg
Acute/chronic physical dependence studies: 0.1-1.0 mg/kg/0.032-1.0 mg/kg
Administration: Intraperitoneal injection (i.p.); single dose
Result: Dose-dependently decreased the effects of morphine in assays of antinociception and locomotor activity.
Did not stimulate locomotor activity or produce antinociception by itself. Could precipitate withdrawal in opioid-dependent mice.
Clinical Trial
分子量

339.43

Formula

C21H25NO3
CAS 号
性状

固体

颜色

White to off-white

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
细胞实验： 

DMSO 中的溶解度 : 175 mg/mL (515.57 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9461 mL 14.7306 mL 29.4612 mL
5 mM 0.5892 mL 2.9461 mL 5.8922 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Nalmefene 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9461 mL 14.7306 mL 29.4612 mL 73.6529 mL
5 mM 0.5892 mL 2.9461 mL 5.8922 mL 14.7306 mL
10 mM 0.2946 mL 1.4731 mL 2.9461 mL 7.3653 mL
15 mM 0.1964 mL 0.9820 mL 1.9641 mL 4.9102 mL
20 mM 0.1473 mL 0.7365 mL 1.4731 mL 3.6826 mL
25 mM 0.1178 mL 0.5892 mL 1.1784 mL 2.9461 mL
30 mM 0.0982 mL 0.4910 mL 0.9820 mL 2.4551 mL
40 mM 0.0737 mL 0.3683 mL 0.7365 mL 1.8413 mL
50 mM 0.0589 mL 0.2946 mL 0.5892 mL 1.4731 mL
60 mM 0.0491 mL 0.2455 mL 0.4910 mL 1.2275 mL
80 mM 0.0368 mL 0.1841 mL 0.3683 mL 0.9207 mL
100 mM 0.0295 mL 0.1473 mL 0.2946 mL 0.7365 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nalmefene55096-26-9Opioid ReceptorApoptosisReactive Oxygen Species (ROS)NO SynthaseToll-like Receptor (TLR)p38 MAPKNF-κBNitric oxide synthasesNOSNuclear factor-κBNuclear factor-kappaBopioid overdosealcohol dependenceopioid antagonistprimary cultured astrocytesRAW264.7 cellsApoE KO miceInhibitorinhibitorinhibit

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