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

Naldemedine tosylate  (Synonyms: S-297995 tosylate)

Cat. No.: HY-19627A Purity: 92.16%
COA Handling Instructions

Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA). Naldemedine tosylate 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 tosylate is predicted to bind to 3CLpro encoded by SARS-CoV2 genome.

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

Naldemedine tosylate Chemical Structure

Naldemedine tosylate Chemical Structure

CAS No. : 1345728-04-2

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Based on 1 publication(s) in Google Scholar

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Description

Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA)[1]. Naldemedine tosylate 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 tosylate is predicted to bind to 3CLpro encoded by SARS-CoV2 genome[3].

IC50 & Target

μ Opioid Receptor/MOR

 

In Vivo

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

MedChemExpress (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 inhibition of small intestinal transit in rats with an ED50 of 0.03 mg/kg
Clinical Trial
Molecular Weight

742.84

Formula

C39H42N4O9S

CAS No.
Appearance

Solid

Color

Off-white to light yellow

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.CC9=CC=C(S(=O)(O)=O)C=C9

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Purity & Documentation
References
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Naldemedine tosylate Related Classifications

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    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 tosylate
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