EST73502 hydrochloride 是一种选择性的，具有口服活性的，可透过血脑屏障的 μ-opioid 受体 (μ-opioid receptor/MOR) 激动剂和 σ1 受体(σ1R) 拮抗剂，对 MOR 和 σ1R 作用的 Ki 值分别为 64 nM 和 118 nM。EST73502 hydrochloride 具有镇痛活性。
货号:ajcx34746
CAS:2535970-65-9
分子式:C19H27ClF2N2O2
分子量：388.88
溶解度:DMSO : 50 mg/mL (128.57 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.