产品
编 号:F128684
分子式:C39H42N4O9S
分子量:742.84
产品类型
结构图
CAS No: 1345728-04-2
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产品详情
生物活性:
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.
体内研究:
Naldemedine tosylate (oral gavage; 0.03-10 mg/kg; once) represses the opioid-induced inhibition of small intestinal transit in rats.Animal Model:6-week-old Wistar and SD male rats
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