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首页-小分子抑制剂&激动剂-GPCR-Cannabinoid Receptor-Z8526711350
Z8526711350

Chemical Structure : Z8526711350

CAS No.: 3069879-24-6 (Rac)

Z8526711350 (CB1R agonist '1350)

货号: PC-24486Not For Human Use, Lab Use Only.

Z8526711350 (CB1R agonist '1350) is a potent, specific agonist of cannabinoid-1 receptor (CB1R) with Ki of 0.95 nM, is a full agonist of CB1R-mediated Gi/o signaling.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Z8526711350 (CB1R agonist '1350) is a potent, specific agonist of cannabinoid-1 receptor (CB1R) with Ki of 0.95 nM, is a full agonist of CB1R-mediated Gi/o signaling.
'1350 shows no strong functional selectivity or bias but is both more potent and relatively more efficacious than CP-55,940 at CB1R but not CB2R.
'1350 is approximately 2-fold more relatively efficacious at recruiting Gi/o and G13 subtypes in CB1R than CP-55,940.
'1350 is strongly analgesic in male mice, with a 2-20-fold therapeutic window over hypolocomotion, sedation, and catalepsy and no observable conditioned place preference.

物理化学性质&存储条件

分子量 437.44
分子式 C20H18F3N3O3S
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

methyl (R)-2-(5-methyl-1-(3-(trifluoromethyl)phenyl)-1H-pyrazole-3-carboxamido)-2-(thiophen-2-yl)propanoate

参考文献

1. Tummino TA, et al. Nat Commun. 2025 Mar 6;16(1):2237.

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