BRD5814 |CAS:1953181-29-7 Probechem Biochemicals

Chemical Structure : BRD5814

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BRD5814 (BRD-5814;BRD 5814)

货号: PC-63349Not For Human Use, Lab Use Only.

BRD5814 is a potent, selective, highly brain penetrant β-arrestin biased dopamine D2 receptor (D2R) antagonist with Ki of 0.27 uM.

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生物&药学活性

BRD5814 is a potent, selective, highly brain penetrant β-arrestin biased dopamine D2 receptor (D2R) antagonist with Ki of 0.27 uM.
BRD5814 strongly diminish D2R/β-arrestin signaling (EC50=0.54 uM) without affecting D2R/Gαi signaling.
BRD5814 demonstrates good target engagement via PET imaging, achieving efficacy in an amphetamine-induced hyperlocomotion mouse model with strongly reduced motoric side effects in a rotarod performance test.

物理化学性质&存储条件

分子量	413.865
分子式	C21H23ClF3NO2
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	4-(4-chlorophenoxy)-4-methyl-1-(2-(2-(trifluoromethyl)phenoxy)ethyl)piperidine

参考文献

1. Weïwer M, et al. ACS Chem Biol. 2018 Apr 20;13(4):1038-1047.

BRD5814 (BRD-5814;BRD 5814)

生物&药学活性

物理化学性质&存储条件

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BRD5814 (BRD-5814;BRD 5814)

生物&药学活性

物理化学性质&存储条件

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