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首页-小分子抑制剂&激动剂-GPCR-Opioid Receptor-PIPE-3297
PIPE-3297

Chemical Structure : PIPE-3297

CAS No.:

PIPE-3297 (PIPE3297)

货号: PC-21712Not For Human Use, Lab Use Only.

PIPE-3297 is a fully efficacious and selective kappa opioid receptor (KOR) agonist with functional GTPγS EC50 of 1.1 nM, Emax=91%, does not elicit β-arrestin-2 recruitment functional response.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PIPE-3297 is a fully efficacious and selective kappa opioid receptor (KOR) agonist with functional GTPγS EC50 of 1.1 nM, Emax=91%, does not elicit β-arrestin-2 recruitment functional response.
PIPE-3297 displays 40- and 600-fold selectivity for the KOR over the related MOR and delta opioid receptor (DOR) respectively.
PIPE-3297 effectively induced oligodendrocyte progenitor cells (OPCs) differentiation of isolated rat OPCs, reaching 90% of T3-control differentiation.
PIPE-3297 (3 and 30 mg/kg, s.c.) reduced the disease score in the mouse experimental autoimmune encephalomyelitis (EAE) model.

物理化学性质&存储条件

分子量 350.51
分子式 C23H30N2O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(2-((1-Benzylazetidin-3-yl)(cyclobutylmethyl)amino)ethyl)phenol

参考文献

1. Thomas O Schrader, et al. ACS Chem Neurosci. 2024 Jan 24. doi: 10.1021/acschemneuro.3c00807.

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