NALDEMEDINE
Naldemedine is a peripherally acting μ‑opioid receptor antagonist that counteracts opioid‑induced constipation without reducing central analgesia. It works by blocking opioids in the gut while sparing the brain. Benefits include improved bowel function and increased spontaneous bowel movements. Side effects include abdominal pain, diarrhea, nausea, flatulence, and, rarely, opioid withdrawal‑like symptoms.
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Product Description
Mechanism of Action
NALDEMEDINE (ID 26816) exhibits a multi‑vector biochemical action pattern, influencing enzymatic cascades, receptor‑mediated 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, second‑messenger systems (cAMP, Ca²⁺, IP₃), ROS generation, membrane polarization and metabolic‑flux channeling.
Depending on biological context, NALDEMEDINE may alter mitochondrial membrane potential, redox buffering capacity, calcium sequestration, cytoskeletal integrity, vesicle trafficking efficiency and transcription‑factor 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:
- High‑resolution receptor–ligand mapping and affinity prediction
- Enzyme‑kinetic profiling and catalytic‑pathway deconstruction
- Mitochondrial‑stress testing, ATP‑flux analysis and ROS‑equilibrium studies
- Integrated multi‑omics research: transcriptomics, metabolomics, proteomics, phosphoproteomics
- Cytoskeletal modelling involving actin/tubulin regulation
- Apoptosis, autophagy, necroptosis and ferroptosis signalling investigations
- Structure–activity relationship (SAR) exploration and molecular optimisation
- Pharmacodynamic simulations for mechanistic threshold and dose‑response studies
Side Effects and Risks
Possible laboratory‑observed risks include:
- Redox imbalance with elevated ROS levels
- Mitochondrial overactivation or respiratory‑chain suppression
- Ion‑channel dysregulation affecting Na⁺/K⁺/Ca²⁺ flow
- Cross‑activation or inhibition of unintended receptor systems
- Cytoskeletal destabilisation and impaired membrane integrity
- Dose‑dependent 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.
Datasheet
| Molecular Formula | C30H34N4O6 |
|---|---|
| Molecular Weight | 570.6 g/mol |
| CAS Number | 916072-89-4 |
| Storage Condition | Store in a cool, dry place. Keep container tightly closed. Protect from moisture and light. |
| Solubility | Slightly soluble |
| Purity | Purity information is available upon request (COA). |
| Synonym | NALDEMEDINE; 916072-89-4; 03KSI6WLXH; naldemedina; S-297995 |
| IUPAC/Chemical Name | (4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,7,9-trihydroxy-N-[2-(3-phenyl-1,2,4-oxadiazol-5-yl)propan-2-yl]-1,2,4,5,7a,13-hexahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamide |
| InChl Key | AXQACEQYCPKDMV-RZAWKFBISA-N |
| InChl Code | InChI=1S/C32H34N4O6/c1-30(2,29-33-27(35-42-29)18-6-4-3-5-7-18)34-28(39)20-15-32(40)22-14-19-10-11-21(37)25-23(19)31(32,26(41-25)24(20)38)12-13-36(22)16-17-8-9-17/h3-7,10-11,17,22,26,37-38,40H,8-9,12-16H2,1-2H3,(H,34,39)/t22-,26+,31+,32-/m1/s1 |
| References |
3D Conformer.
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