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β2AR-IN-15

Chemical Structure : β2AR-IN-15

CAS No.: 2088234-50-6

β2AR-IN-15

Catalog No.: PC-70285Not For Human Use, Lab Use Only.

An allosteric, small-molecule negative modulator for β2AR with Kd of 1.7 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

An allosteric, small-molecule negative modulator for β2AR with Kd of 1.7 uM; binds in proximity to the G-protein binding site on the cytosolic surface of the β2AR; inhibits cAMP production through the β2AR, but not that mediated by other Gs-coupled receptors; also similarly inhibits β-arrestin recruitment to the activated β2AR.

Physicochemical Properties

M.Wt 647.614
Formula C34H39BrN4O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((2S)-3-(((S)-3-(3-bromophenyl)-1-(methylamino)-1-oxopropan-2-yl)amino)-2-(2-cyclohexyl-2-phenylacetamido)-3-oxopropyl)benzamide

References

1. Ahn S, et al. Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):1708-1713.

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