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首页-小分子抑制剂&激动剂-GPCR-Cannabinoid Receptor-ISAM-CG557
ISAM-CG557

Chemical Structure : ISAM-CG557

CAS No.:

ISAM-CG557

货号: PC-25356Not For Human Use, Lab Use Only.

ISAM-CG557 is a potent, selective, and functionally biased CB2 receptor (CB2R) agonist with binding Ki of 54.6 nM, with negligible binding to CB1R, shows strongly biased toward MAPK signaling.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ISAM-CG557 is a potent, selective, and functionally biased CB2 receptor (CB2R) agonist with binding Ki of 54.6 nM, with negligible binding to CB1R, shows strongly biased toward MAPK signaling.
ISAM-CG557 display notable bias toward MAPK, especially in β-arrestin-MAPK signaling, indicating a selective MAPK pathway activation.
ISAM-CG557 shows EC50 of 0.60 nM and Emax = 60% for CB2R activity.
ISAM-CG557 significantly reduced the production of pro-inflammatory cytokines (TNF-α, IFN-γ, IL-1β, and IL-6) in unstimulated monocytes and macrophages.
ISAM-CG557 elicites a concentration-dependent neuroprotective effect on neurite length in transfected SH-SY5Y cells.

物理化学性质&存储条件

分子量 380.42
分子式 C21H21FN4O2
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

(S)-1-(1-(4-fluorobenzyl)-1H-indazole-3-carbonyl)piperidine-2-carboxamide

参考文献

1. Gioé-Gallo C, et al. J Med Chem. 2025 Aug 12. doi: 10.1021/acs.jmedchem.5c00604.

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