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Product Description
– Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA)[1]. 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[2]. Naldemedine can be used in opioid-induced constipation (OIC) research[2]. Naldemedine is predicted to bind to 3CLpro encoded by SARS-CoV2 genome[3].
Web ID
– HY-19627
Shipping
– Room temperature
Applications
– Neuroscience-Neuromodulation
Molecular Formula
– C32H34N4O6
References
– [1]Hannah A. Blair. Naldemedine: A Review in Opioid-Induced Constipation. Drugs. 2019 Jul;79(11):1241-1247.|[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.|[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.
CAS Number
– 916072-89-4
Molecular Weight
– 570.64
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
Clinical Information
– Launched
Research Area
– Metabolic Disease; Neurological Disease
Solubility
– 10 mM in DMSO
Target
– Opioid Receptor
Isoform
– μ Opioid Receptor/MOR
Pathway
– GPCR/G Protein;Neuronal Signaling
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
