Biological Activity
ML382 is a potent, selective, positive allosteric modulator of Mas-related G protein-coupled receptor X1 (MrgprX1) with EC50 of 190 nM in cell based Ca2+ imaging assay; displays >100-fold selectivity versus MrgX2; enhances the ability of BAM8-22 to inhibit high-voltage-activated Ca2+ channels and attenuates spinal nociceptive transmission; effectively attenuated evoked, persistent, and spontaneous pain without causing obvious side effects; attenuates both evoked pain hypersensitivity and spontaneous pain in MrgprX1 mice; an invaluable research tool to study the role of MrgprX1 in chronic pain.
In Vitro
No in vitro data are provided in the current product source. Contact us for further information.
In Vivo
No in vivo data are provided in the current product source. Contact us for further information.
References & source
[1]. Li Z, et al. Targeting human Mas-related G protein-coupled receptor X1 to inhibit persistent pain. Proc Natl Acad Sci U S A. 2017;114(10):E1996-E2005.
[2]. Wen W, et al. Discovery and characterization of 2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.
