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

Naldemedine tosylate  (Synonyms: S-297995 tosylate)

目录号: HY-19627A 纯度: 92.16%
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Naldemedine (S-297995) tosylate 是一种具有口服活性的 μ-阿片受体拮抗剂 (PAMORA)。Naldemedine tosylate 对重组人源 μ-、δ- 和 κ- 阿片受体表现出强大的亲和作用 (Ki 分别为 0.34，0.43，0.94 nM) 和拮抗作用 (IC50 分别为 25.57，7.09，16.1 nM) 。Naldemedine tosylate 可用于阿片类化合物引起的便秘 (OIC) 研究。Naldemedine tosylate 预测可能与 SARS-CoV2 基因组编码的 3CLpro 结合。

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Naldemedine tosylate Chemical Structure

Naldemedine tosylate Chemical Structure

CAS No. : 1345728-04-2

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规格 价格 是否有货 数量
1 mg ￥2100
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5 mg ￥4620
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10 mg ￥7400
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Other Forms of Naldemedine tosylate:

Naldemedine tosylate 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体内研究
(In Vivo)

Naldemedine tosylate (oral gavage; 0.03-10 mg/kg; once) represses the opioid-induced inhibition of small intestinal transit in rats[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 inhibition of small intestinal transit in rats with an ED50 of 0.03 mg/kg
Clinical Trial
分子量

742.84

Formula

C39H42N4O9S
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

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

纯度 & 产品资料
参考文献

Naldemedine tosylate 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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.

Keywords:

Naldemedine1345728-04-2S-297995S297995S 297995Opioid Receptoropioid-induced constipationμ-opioid receptorOICSARS-CoV2Inhibitorinhibitorinhibit

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