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首页-小分子抑制剂&激动剂-GPCR-Opioid Receptor-HSK21542
HSK21542

Chemical Structure : HSK21542

CAS No.: 2269511-95-5

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HSK21542 (Anrikefon, HSK-21542)

货号: PC-23826Not For Human Use, Lab Use Only.

Anrikefon (HSK21542) is a potent, selective and peripherally-restricted kappa opioid receptor (KOR) agonist, prevents [3H]diprenorphine binding to KOR with IC50 of 0.54 nM, and binding Kd of 0.068 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Anrikefon (HSK21542) is a potent, selective and peripherally-restricted kappa opioid receptor (KOR) agonist, prevents [3H]diprenorphine binding to KOR with IC50 of 0.54 nM, and binding Kd of 0.068 nM.
HSK21542 significantly inhibits forskolin-induced cAMP accumulation in HEK-293 cells that stably expressed human κ opioid receptor with an EC50 of 2.41 pM.
HSK21542 displays no significant affinity against a broad panel of receptors, ion channels, transporters and enzymes, including MOR and DOR.
HSK21542 significantly inhibits acetic acid-, hindpaw incision- or chronic constriction injury-induced pain-related behaviors in animal models of pain

物理化学性质&存储条件

分子量 703.93
分子式 C39H57N7O5
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

7-(D-phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-2-acetyl-2,7-diazaspiro (3.5)nonane

参考文献

1. Wang X, et al. Front Pharmacol. 2021 Nov 16;12:773204.

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