EST73502

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EST73502

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:

1838622-25-5

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

EST73502 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K_i值分别为 64 nM 和 118 nM。EST73502 可用于缓解疼痛研究。

生物活性

EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dualμ-opioid receptor (MOR)agonist andσ1 receptor (σ1R)antagonist, withK_is of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity^[1].

IC₅₀& Target

Ki: 64 nM (MOR), 118 nM (σ1R)^[1]

体内研究
(In Vivo)

EST73502 (10-40 mg/kg; p.o.) shows a dose-response analgesic effect reaching a maximum of 64% and an EC₅₀of 14 mg/kg in the paw pressure test in CD1 male mice^[1].
EST73502 (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].

Animal Model:	Male CD1 mice, PSNL model^[1]
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection, twice a day, for 10 days
Result:	Attenuated the expression of mechanical allodynia induced by PSNL, reaching a maximal effect of 56%.

分子量

352.42

Formula

C₁₉H₂₆F₂N₂O₂

CAS 号

1838622-25-5

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.