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

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.

For research use only. We do not sell to patients.

Nalmefene Chemical Structure

Nalmefene Chemical Structure

CAS No. : 55096-26-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Nalmefene:

Nalmefene Related Antibodies

Top Publications Citing Use of Products

View All Opioid Receptor Isoform Specific Products:

View All Isoforms
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

View All NO Synthase Isoform Specific Products:

View All Isoforms
nNOS iNOS eNOS

View All Toll-like Receptor (TLR) Isoform Specific Products:

View All Isoforms
TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

View All p38 MAPK Isoform Specific Products:

View All Isoforms
p38 MAPK p38α p38β MAPK13 p38δ p38γ

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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]
In Vitro

Nalmefene (0.01-300 μM; 1.5-3.5 h) can inhibit the production of ROS, the synthesis of iNOS, block the TLR4 signaling pathway, the phosphorylation of MAPKs, and the activation of NF-κB, thereby reducing cell death in primary cultured astrocytes under ethanol stimulation[1].
Nalmefene (0-300 μg/mL; 24 h) can promote the expression of CD36, and reduce the mRNA levels of μ-, δ- and κ-opioid receptors by 73%, 56%, and 39% respectively in RAW264.7 cells[2].

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

Nalmefene Related Antibodies

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.
In Vivo

Nalmefene (0.1 mg/kg; intraperitoneal injection; twice every four days; 2 weeks) can prevent ethanol-induced neuroinflammation, myelin damage, apoptosis, as well as the drinking preference and intake of alcohol in mice[1].
Nalmefene (1-3 mg/kg; subcutaneous injection; 21 days) aggravates the formation of atherosclerotic plaques in ApoE KO mice fed a high-fat diet[2].
Nalmefene (0.032-1 mg/kg; intraperitoneal injection; single-dose) antagonizes the effects of morphine in mice[3].

MedChemExpress (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.
Molecular Weight

339.43

Formula

C21H25NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@]12[C@@]34C5=C(C[C@@]2([H])N(CC6CC6)CC4)C=CC(O)=C5O[C@@]3([H])C(CC1)=C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 175 mg/mL (515.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Nalmefene Related Classifications

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 SpeciesNO SynthaseToll-like Receptor (TLR)p38 MAPKNF-κBNitric oxide synthasesNOSNuclear factor-κBNuclear factor-kappaBopioid overdosealcohol dependenceopioid antagonistprimary cultured astrocytesRAW264.7 cellsApoE KO miceInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Nalmefene
Cat. No.:
HY-107744
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB) Italian - IT (393 KB) Portuguese - PT (393 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.