Cat. No.: HY-107744

Nalmefene

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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.

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Pureté: 99.94%
CAS No.: 55096-26-9
Formule: C₂₁H₂₅NO₃
Masse moléculaire:339.43

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Nalmefene Chemical Structure

CAS No.: 55096-26-9

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

MOR, DOR, KOR^[2]

Voir tous les produits spécifiques à Isoform Opioid Receptor :

Voir tous les produits spécifiques à Isoform NO Synthase :

Voir tous les produits spécifiques à Isoform Toll-like Receptor (TLR) :

Voir tous les produits spécifiques à Isoform p38 MAPK :

Voir tous les produits spécifiques à Isoform NF-κB :

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.

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 55096-26-9
Appearance Solid
Masse moléculaire 339.43
Formule C₂₁H₂₅NO₃
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Patent

US20210023074A1.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (294.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9461 mL

14.7306 mL

29.4612 mL

5 mM

0.5892 mL

2.9461 mL

5.8922 mL

10 mM

0.2946 mL

1.4731 mL

2.9461 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (287 KB)
SDS (393 KB)
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- Deutsch - DE (393 KB)
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- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Montesinos J, et al. Nalmefene Prevents Alcohol-Induced Neuroinflammation and Alcohol Drinking Preference in Adolescent Female Mice: Role of TLR4. Alcohol Clin Exp Res. 2017 Jul;41(7):1257-1270. [Content Brief]

[2]. Koga M, et al. Nalmefene, an opioid receptor modulator, aggravates atherosclerotic plaque formation in apolipoprotein E knockout mice by enhancing oxidized low-density lipoprotein uptake in macrophages. Biochem Biophys Rep. 2024 Mar 23;38:101688. [Content Brief]

[3]. Osborn MD, et al. In vivo characterization of the opioid antagonist nalmefene in mice. Life Sci. 2010 Apr 10;86(15-16):624-30. [Content Brief]

[4]. Wang DS, et al. Nalmefene: a long-acting opioid antagonist. Clinical applications in emergency medicine. J Emerg Med. 1998 May-Jun;16(3):471-5. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Nalmefene

1 Cited Publications

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