β-Funaltrexamine
Based on 2 publication(s) in Google Scholar
β-Funaltrexamine (β-FNA) is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases.
For research use only. We do not sell to patients.
- CAS No.: 72782-05-9
- Formula: C25H30N2O6
- Molecular Weight:454.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) β-Funaltrexamine
MoreAll Opioid Receptor Isoforms
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Biological Activity
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μ Opioid Receptor/MOR |
iNOS |
NF-κB |
TLR4 |
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Cell Line
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Type | Value | Description | References |
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| Caco-2 | Inhibition |
0.49 %
Compound: BETA-FUNALTREXAMINE
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Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
β-Funaltrexamine (0.3-100 μM; 24 h) concentration-dependently inhibits IL-1β-induced CXCL10 protein expression in normal human astrocytes with an EC50 of 7.6 μM, with greater inhibitory efficacy when combined with the ubiquitin-activating enzyme E1 inhibitor PYR41[2].
β-Funaltrexamine (10 μM; 8 h) significantly inhibits IL-1β-induced CXCL10 mRNA expression in normal human astrocytes after 8 h of co-incubation[2].
β-Funaltrexamine (10 μM; 60 min pre-treatment/remainder of 24 h total incubation) produces persistent, washout-resistant inhibition of IL-1β-induced CXCL10 expression in normal human astrocytes, and can inhibit CXCL10 expression when added 6 h after initial IL-1β stimulation[2].
β-Funaltrexamine (10 μM; 10, 30 min) significantly inhibits IL-1β-induced p38 MAPK activation in normal human astrocytes at 10 and 30 min of co-incubation[2].
β-Funaltrexamine (10 μM; 90, 270 min) significantly inhibits IL-1β-induced A20 protein expression in normal human astrocytes at 90 and 270 min of co-incubation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
β-Funaltrexamine (28 mg/kg; i.p.; single injection) significantly inhibits LPS-induced brain CXCL10 expression in male C57BL/6J mice, demonstrating anti-inflammatory activity in a neuroinflammation model[2].
β-FNA (12.5-50 mg/kg; i.p.; single dose) significantly inhibits LPS-induced CXCL10 and CCL2 expression in the brain of male C57BL/6J mice, and the 50 mg/kg dose prevents LPS-induced reductions in locomotor activity[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 72782-05-9
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Molecular Weight 454.52
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Formula C25H30N2O6
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SMILES
O[C@]12[C@@]34C5=C(C[C@@]2([H])N(CC4)CC6CC6)C=CC(O)=C5O[C@@]3([H])[C@@H](CC1)NC(/C=C/C(OC)=O)=O
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Synonyms
β-FNA
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Sci Adv
2026 Feb 13;12(7):eaea9832. PMID: 41671375 -
Purity & Documentation
References
[1]. Wu CC, et al. β-Funaltrexamine Displayed Anti-inflammatory and Neuroprotective Effects in Cells and Rat Model of Stroke. Int J Mol Sci. 2020;21(11):3866. Published 2020 May 29. [Content Brief]
[2]. Davis RL, et al. The opioid antagonist, β-funaltrexamine, inhibits NF-κB signaling and chemokine expression in human astrocytes and in mice. Eur J Pharmacol. 2015;762:193-201. [Content Brief]
[3]. Davis RL, et al. The opioid antagonist, β-funaltrexamine, inhibits lipopolysaccharide-induced neuroinflammation and reduces sickness behavior in mice. Physiol Behav. 2017;173:52-60. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
β-Funaltrexamine Related Classifications
HY-160938 Related Classifications
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