NALFURAFINE
Nalfurafine is a selective opioid receptor agonist used to treat intractable pruritus, particularly in patients with chronic liver or kidney disease. It modulates itch pathways in the central nervous system. Benefits include significant itch reduction and improved sleep. Side effects include insomnia, dizziness, nausea, fatigue, dysphoria, and, occasionally, hallucinations or mood changes. Only GMP materials will be supplied, logistics all according to GDP.
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Product Description
Mechanism of Action
NALFURAFINE exhibits a multivector biochemical action pattern, influencing enzymatic cascades, receptormediated signalling, intracellular ion behaviour, mitochondrial oxidative dynamics and transcriptional regulatory networks. Its structural characteristics suggest interaction with catalytic residues, allosteric pockets and regulatory scaffolds, enabling modulation of phosphorylation circuits, secondmessenger systems (cAMP, Ca²⁺, IP), ROS generation, membrane polarization and metabolicflux channeling.
Depending on biological context, NALFURAFINE may alter mitochondrial membrane potential, redox buffering capacity, calcium sequestration, cytoskeletal integrity, vesicle trafficking efficiency and transcriptionfactor activation, resulting in broad mechanistic adaptability across experimental systems.
Benefits and Advantages
This compound is highly valued in advanced biochemical and pharmacological research frameworks, including:
- Highresolution receptorligand mapping and affinity prediction
- Enzymekinetic profiling and catalyticpathway deconstruction
- Mitochondrialstress testing, ATPflux analysis and ROSequilibrium studies
- Integrated multiomics research: transcriptomics, metabolomics, proteomics, phosphoproteomics
- Cytoskeletal modelling involving actin/tubulin regulation
- Apoptosis, autophagy, necroptosis and ferroptosis signalling investigations
- Structureactivity relationship (SAR) exploration and molecular optimisation
- Pharmacodynamic simulations for mechanistic threshold and doseresponse studies
Side Effects and Risks
Possible laboratoryobserved risks include:
- Redox imbalance with elevated ROS levels
- Mitochondrial overactivation or respiratorychain suppression
- Ionchannel dysregulation affecting Na⁺/K⁺/Ca²⁺ flow
- Crossactivation or inhibition of unintended receptor systems
- Cytoskeletal destabilisation and impaired membrane integrity
- Dosedependent cytotoxicity or induction of apoptotic/autophagic pathways
- Transcriptional instability and activation of inflammatory cascades (NF-κB, JNK, p38)
Strict biosafety handling, controlled dosing and regulated environmental conditions are required for all experimental use. Not intended for human or veterinary application.
Only GMP materials will be supplied, logistics all according to GDP.
Datasheet
| Molecular Formula | C16H19Cl2NO3 |
|---|---|
| Molecular Weight | 476.6 g/mol |
| CAS Number | 152657-84-6 |
| Storage Condition | Store in a cool, dry place. Keep container tightly closed. Protect from moisture and light. |
| Solubility | Solubility depends on solvent and conditions (e.g., pH). Please contact us for solvent-specific guidance. |
| Purity | Purity information is available upon request (COA). |
| Synonym | Nalfurafine; 152657-84-6; nalfurafina; TRK 820; XC41AVD567 |
| IUPAC/Chemical Name | (E)-N-[(4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]-3-(furan-3-yl)-N-methylprop-2-enamide |
| InChl Key | XGZZHZMWIXFATA-UEZBDDGYSA-N |
| InChl Code | InChI=1S/C28H32N2O5/c1-29(23(32)7-4-18-9-13-34-16-18)20-8-10-28(33)22-14-19-5-6-21(31)25-24(19)27(28,26(20)35-25)11-12-30(22)15-17-2-3-17/h4-7,9,13,16-17,20,22,26,31,33H,2-3,8,10-12,14-15H2,1H3/b7-4+/t20-,22-,26+,27+,28-/m1/s1 |
| References |
3D Conformer.
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