Naldemedine
Based on 2 publication(s) in Google Scholar
Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA). Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine can be used in opioid-induced constipation (OIC) research. Naldemedine is predicted to bind to 3CLpro encoded by SARS-CoV2 genome.
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- No. CAS: 916072-89-4
- Fòrmula: C32H34N4O6
- Peso molecular:570.64
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Almacenamiento:
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Actividad biológica
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Naldemedine
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Actividad biológica
Descripciòn
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-week-old Wistar and SD male rats[2]
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Dosage:0.03-10 mg/kg
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Administration:Oral gavage; 0.03-10 mg/kg; once
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Result:Repressed the subcutaneous morphine-induced inhibition of small intestinal transit in rats with an ED50 of 0.03 mg/kg, and the oxycodone-induced inhibition model with an ED50 of 0.02 mg/kg.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 916072-89-4
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Peso molecular 570.64
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Fòrmula C32H34N4O6
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SMILES
O[C@@]1(CC(C(NC(C)(C2=NC(C3=CC=CC=C3)=NO2)C)=O)=C4O)[C@@]([C@@]4([H])OC5=C6O)(CC7)C5=C(C=C6)C[C@@]1([H])N7CC8CC8
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Synonyms
S-297995
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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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Free Radic Biol Med
Targeted delivery of nebivolol via lactoferrin-modified liposomes inhibits NEK7-mediated pyroptosis to ameliorate inflammatory bowel disease. [Abstract]2026 Aug 16:252:493-508. PMID: 42061481 -
Biofactors
GRHL2/SENP1/VDR Signaling Axis: A Key Regulator of SUMOylation and Calcitriol Resistance in SHPT. [Abstract]2026 Mar-Apr;52(2):e70086. PMID: 41760369
Pureza y Documentación
Referencias
[1]. Hannah A. Blair. Naldemedine: A Review in Opioid-Induced Constipation. Drugs. 2019 Jul;79(11):1241-1247. [Content Brief]
[2]. Toshiyuki Kanemasa, et al. Pharmacologic effects of naldemedine, a peripherally acting μ-opioid receptor antagonist, in in vitro and in vivo models of opioid-induced constipation. Neurogastroenterol Motil. 2019 May;31(5):e13563. [Content Brief]
[3]. Sugandh Kumar, et al. Identification of multipotent drugs for COVID-19 therapeutics with the evaluation of their SARS-CoV2 inhibitory activity. Comput Struct Biotechnol J. 2021;19:1998-2017. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Naldemedine Related Classifications
HY-19627 Related Classifications
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