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Naldemedine tosylate

目录号 : GC71539

Naldemedine tosylate是一种口服活性μ阿片受体拮抗剂(PAMORA)。

Naldemedine tosylate Chemical Structure

Cas No.:1345728-04-2

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1 mg
¥1,890.00
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5 mg
¥4,158.00
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10 mg
¥6,660.00
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Sample solution is provided at 25 µL, 10mM.

Description

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.

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

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.

化学性质

Cas No. 1345728-04-2 SDF
分子式 C39H42N4O9S 分子量 742.84
溶解度 DMSO : 100 mg/mL (134.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) 储存条件 -20°C, stored under nitrogen, away from moisture
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 1.3462 mL 6.7309 mL 13.4618 mL
5 mM 0.2692 mL 1.3462 mL 2.6924 mL
10 mM 0.1346 mL 0.6731 mL 1.3462 mL
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