β2AR-IN-15 

β2AR-IN-15 is a selective β2-adrenergic receptor (β2AR) antagonist with a K_d of 1.7 μM. β2AR-IN-15 binds to an intracellular β2AR region overlapping the G-protein binding site, enhancing orthosteric inverse agonist binding while negatively modulating binding of orthosteric agonists with EC₅₀ values of 1.9 and 0.48 μM. β2AR-IN-15 shows inhibitory effect on cAMP production and β-arrestin recruitment to activated β2AR. β2AR-IN-15 can be used for the research of cardiovascular and pulmonary diseases^[1].

β2AR-IN-15 (Compound 15) acts as a negative allosteric modulator for human β2AR reconstituted in nanodiscs, decreasing orthosteric agonist binding with an EC₅₀ of 1.9 μM and increasing inverse agonist binding with an EC₅₀ of 0.48 μM^[1].
β2AR-IN-15 binds directly to purified human β2AR with a K_d of 1.7 μM and a 1:1 binding stoichiometry^[1].
β2AR-IN-15 competes with the intracellular-binding nanobody Nb60 for binding to human β2AR, indicating its binding site is located on the receptor's intracellular region^[1].
β2AR-IN-15 inhibits transducer-promoted high-affinity agonist binding to human β2AR reconstituted in nanodiscs, with EC₅₀ values of 2.8 μM for Gαβγ and 2.2 μM for β-arrestin1, showing no bias between the two transducers^[1].
β2AR-IN-15 (1.25-50 μM; 20 min) inhibits isoproterenol-stimulated cAMP production in HEK-293 cells with endogenous β2AR and β-arrestin recruitment to chimeric β2V₂R, causing 7.1-fold and 7.4-fold right shifts of the isoproterenol EC₅₀, respectively^[1].
β2AR-IN-15 (1.25-50 μM; 20 min) selectively inhibits agonist-stimulated β-arrestin recruitment to human β2AR, with significantly reduced or no activity on β1AR, V₂R, VIPR, and AT₁R^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

647.60

C₃₄H₃₉BrN₄O₄

2088234-50-6

Solid

O=C(N)C1=CC=C(C[C@H](NC(C(C2CCCCC2)C3=CC=CC=C3)=O)C(N[C@@H](CC4=CC=CC(Br)=C4)C(NC)=O)=O)C=C1

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Ahn S, et al. Allosteric "beta-blocker" isolated from a DNA-encoded small molecule library. Proc Natl Acad Sci U S A. 2017;114(7):1708-1713.