Naldemedine

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Naldemedine

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	916072-89-4
包装:	5mg
市场价:	41000元

S-297995

Naldemedine (S-297995) 是一种具有口服活性的 μ-阿片受体拮抗剂 (PAMORA)。Naldemedine 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 可用于阿片类化合物引起的便秘 (OIC) 研究。Naldemedine 预测可能与 SARS-CoV2 基因组编码的 3CL^pro结合。

生物活性

Naldemedine (S-297995) is an orally activeμ-opioid receptorantagonist (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 3CL^proencoded by SARS-CoV2 genome^[3].

体内研究
(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].

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 ED₅₀of 0.03 mg/kg, and the oxycodone-induced inhibition model with an ED₅₀of 0.02 mg/kg.

Clinical Trial

分子量

570.64

Formula

C₃₂H₃₄N₄O₆

CAS 号

916072-89-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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