1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. Naldemedine

Naldemedine  (Synonyms: S-297995)

Cat. No.: HY-19627
Handling Instructions

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.

For research use only. We do not sell to patients.

Naldemedine Chemical Structure

Naldemedine Chemical Structure

CAS No. : 916072-89-4

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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].

In Vivo

Naldemedine (oral gavage; 0.03-10 mg/kg; once) represses the opioid-induced inhibition of small intestinal transit in rats by subcutaneous morphine and oxycodone[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-week-old Wistar and SD male rats[2]
Dosage: 0.03-10 mg/kg
Administration: Oral gavage; 0.03-10 mg/kg; once
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.
Clinical Trial
Molecular Weight

570.64

Formula

C32H34N4O6

CAS No.
SMILES

O[[email protected]@]1(CC(C(NC(C)(C2=NC(C3=CC=CC=C3)=NO2)C)=O)=C4O)[[email protected]@]([[email protected]@]4([H])OC5=C6O)(CC7)C5=C(C=C6)C[[email protected]@]1([H])N7CC8CC8

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Naldemedine
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HY-19627
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