Arrestin

Other GPCR & G Protein Related Inhibitors

Hedgehog/Smoothened PKA CGRP Receptor Endothelin Receptor S1P Receptor Cannabinoid Receptor SGLT Opioid Receptor GPR CCR

Cat.No.	Product Name	Information	Product Use Citations	Product Validations
E1242^New	Barbadin	Barbadin is a selective β-arrestin/β2-adaptin interaction inhibitor with IC50 values of 19.1 μM (β-arrestin1) and 15.6 μM (β-arrestin2). It inhibits agonist-induced endocytosis of β2-adrenergic, V2-vasopressin, and angiotensin-II type-1 receptors. Additionally, Barbadin exhibits pro-apoptotic activity.
S8695	ML221	ML221 is a potent apelin receptor (APJ) functional antagonist in cell-based assays that is >37-fold selective over the closely related angiotensin II type 1 (AT1) receptor. The IC50 values of ML221 are 0.70 and 1.75 μM in a cAMP assay and β-arrestin assay, respectively.	Nat Commun, 2022, 13(1):4229 J Mol Cell Cardiol, 2021, S0022-2828(21)00246-7 Research Square, 2021, 10.21203/rs.3.rs-916525/v1

Cat.No.

Product Name

Information

Product Use Citations

Product Validations

E1242^New

Barbadin

Barbadin is a selective β-arrestin/β2-adaptin interaction inhibitor with IC50 values of 19.1 μM (β-arrestin1) and 15.6 μM (β-arrestin2). It inhibits agonist-induced endocytosis of β2-adrenergic, V2-vasopressin, and angiotensin-II type-1 receptors. Additionally, Barbadin exhibits pro-apoptotic activity.

S8695

ML221

ML221 is a potent apelin receptor (APJ) functional antagonist in cell-based assays that is >37-fold selective over the closely related angiotensin II type 1 (AT1) receptor. The IC50 values of ML221 are 0.70 and 1.75 μM in a cAMP assay and β-arrestin assay, respectively.

Nat Commun, 2022, 13(1):4229

J Mol Cell Cardiol, 2021, S0022-2828(21)00246-7

Research Square, 2021, 10.21203/rs.3.rs-916525/v1