RTI-7470-44 | hTAAR1 antagonist | Probechem Biochemicals

Chemical Structure : RTI-7470-44

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RTI-7470-44 (TAAR1 antagonist)

货号: PC-72353Not For Human Use, Lab Use Only.

RTI-7470-44 is a potent, selective human trace amine-associated receptor subtype 1 (hTAAR1) inhibitor with IC50 of 8.4 nM in vitro cAMP functional assay.

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生物&药学活性

RTI-7470-44 is a potent, selective human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with IC50 of 8.4 nM in vitro cAMP functional assay.
RTI-7470-44 exhibits a Ki of 0.3 nM in a radioligand binding assay, and shows species selectivity (>90-fold) for hTAAR1 over the rat and mouse orthologues.
RTI-7470-44 displays good blood–brain barrier permeability, moderate metabolic stability, and a favorable preliminary off-target profile.
RTI-7470-44 increased the spontaneous firing rate of mouse VTA dopaminergic neurons and blocked the effects of the known TAAR1 agonist RO5166017.

物理化学性质&存储条件

分子量	449.836
分子式	C19H11ClF3N5OS
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-((6-(4-chlorophenyl)-3-cyano-4-(trifluoromethyl)pyridin-2-yl)thio)-N-(pyrimidin-2-yl)acetamide

参考文献

1. Ann M Decker, et al. ACS Chem Neurosci. 2022 Mar 24. doi: 10.1021/acschemneuro.2c00086.

RTI-7470-44 (TAAR1 antagonist)

生物&药学活性

物理化学性质&存储条件

参考文献

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RTI-7470-44 (TAAR1 antagonist)

生物&药学活性

物理化学性质&存储条件

参考文献

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