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首页-小分子抑制剂&激动剂-GPCR-Opioid Receptor-Triazole 1.1
Triazole 1.1

Chemical Structure : Triazole 1.1

CAS No.: 1526944-32-0

Triazole 1.1

货号: PC-24299Not For Human Use, Lab Use Only.

Triazole 1.1 is a potent, G protein signaling-biased κ opioid receptor (KOR) agonist with EC50 of 77.2 nM in [35S]GTPγS binding assays, with bias factor (G protein/βarrestin2) of 28.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Triazole 1.1 is a potent, G protein signaling-biased κ opioid receptor (KOR) agonist with EC50 of 77.2 nM in [35S]GTPγS binding assays, with bias factor (G protein/βarrestin2) of 28.
Triazole 1.1 induces KOR-mediated antinociception and suppresses chloroquine phosphate–induced scratching responses in C57BL/6 mice.
Triazole 1.1 does not decrease locomotor activity in mice.
Triazole 1.1 decreases dopamine concentrations in the nucleus accumbens in mice, but not U50,488H.
Triazole 1.1 promotes analgesia in the absence of dysphoria in the rat ICSS model.

物理化学性质&存储条件

分子量 430.45
分子式 C21H17F3N4OS
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

2-(4-(furan-2-ylmethyl)-5-((4-methyl-3-(trifluoromethyl)benzyl)thio)-4H-1,2,4-triazol-3-yl)pyridine

参考文献

1. Brust TF, et al. Sci Signal. 2016 Nov 29;9(456):ra117.

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