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EST73502 hydrochloride
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。
EST73502 hydrochloride图片
CAS NO:2535970-65-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
EST73502 hydrochloride 是一种选择性、口服活性和血脑屏障 (BBB) 渗透双重 μ-阿片受体 (MOR) 激动剂和 σ1 受体 (σ1R) 拮抗剂,对 MOR 和σ1R,分别。
Cas No.2535970-65-9
分子式C19H27ClF2N2O2
分子量388.88
溶解度DMSO : 50 mg/mL (128.57 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

EST73502 hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 hydrochloride has antinociceptive activity[1].

EST73502 hydrochloride (10-40 mg/kg; p.o.) shows a dose-response analgesic effect reaching a maximum of 64% and an EC50 of 14 mg/kg in the paw pressure test in CD1 male mice[1].EST73502 hydrochloride (5 mg/kg; i.p.; twice a day; for 10 days) attenuates partial sciatic nerve ligation (PSNL)-induced mechanical allodynia in male CD1 mice[1].

[1]. MÓnica GarcÍa, et al. Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σ 1 Receptor Antagonist Clinical Candidate for the Treatment of Pain. J Med Chem. 2020 Oct 16.