Barbadin

Chemical Structure : Barbadin

CAS No.: 356568-70-2

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货号: PC-61188Not For Human Use, Lab Use Only.

Barbadin is a small molecule that selectively inhibits the β-arrestin/β2-adaptin interaction (IC50=19.1/15.6 uM for β-arrestin1/2) without effect on the formation of receptor/β-arrestin complexes.

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生物&药学活性

Barbadin is a small molecule that selectively inhibits the β-arrestin/β2-adaptin interaction (IC50=19.1/15.6 uM for β-arrestin1/2) without effect on the formation of receptor/β-arrestin complexes.
Barbadin selectively inhibits the β-arrestin/AP2 interaction.
Barbadin blocks agonist-promoted endocytosis of the prototypical GPCR β2AR, V2R and AT1R, but does not affect β-arrestin-independent (transferrin) or AP2-independent (endothelin-A) receptor internalization.
Barbadin fully blocks V2R-stimulated ERK1/2 activation and blunts cAMP accumulation promoted by both V2R and β2AR.

物理化学性质&存储条件

分子量	333.409
分子式	C19H15N3OS
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	3-Azanyl-5-[4-(phenylmethyl)phenyl]thieno[2,3-d]pyrimidin-4-one

参考文献

1. Beautrait A, et al. Nat Commun. 2017 Apr 18;8:15054.

Barbadin

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Barbadin

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