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首页-小分子抑制剂&激动剂-GPCR-Dopamine Receptor-CAB-01-019
CAB-01-019

Chemical Structure : CAB-01-019

CAS No.: 2826198-44-9

CAB-01-019 (D4R antagonist 16f)

货号: PC-21105Not For Human Use, Lab Use Only.

CAB-01-019 is potent, selective dopamine D4 receptor (D4R) full antagonist with binding Ki of 2.2 nM, >500-fold selectivity over D2R and D3R.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CAB-01-019 is potent, selective dopamine D4 receptor (D4R) full antagonist with binding Ki of 2.2 nM, >500-fold selectivity over D2R and D3R.
CAB-01-019 demonstrates excellent D4R selectivity in functional assays and is a competitive antagonist at D4R.
CAB-01-019 is a potent full D4R antagonist for β-arrestin recruitment with no D4R agonist activity.
CAB-01-019 is a potent low-efficacy D4R partial agonist, metabolically stable in rat and human liver microsomes, and has excellent brain penetration in rats.
CAB-01-019 (5, 15, and 30 mg/kg, i.p.) dose-dependently decreased food-maintained responding in male Fisher F344 rats, decreases iv cocaine self-administration in rats.

物理化学性质&存储条件

分子量 338.47
分子式 C19H22N4S
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-(3-(4-(Pyridin-2-yl)piperazin-1-yl)propyl)benzo[d]thiazole

参考文献

1. Comfort A. Boateng, et al. Journal of Medicinal Chemistry 2023.

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