ML-382

ML-382 is a positive allosteric modulator of MAS-related G protein-coupled receptor family member X1 (MRGPRX1).¹ It potentiates activation of MRGPRX1 induced by the MRGPRX1 agonist BAM 22P (8-22) (Item No. 35263) in HEK293 cells expressing the human receptor (EC₅₀ = 0.19 µM) but does not potentiate activation of MRGPRX2 induced by the MRGPRX2 agonist proadrenomedullin (PAMP) in HEK293 cells expressing the human receptor at 5 µM. ML-382 is also selective for MRGPRX1 over a panel of 68 G protein-coupled receptors (GPCRs), ion channels, and transporters at 10 µM. It enhances inhibition of high-voltage-activated calcium currents (I_Ca ) induced by BAM 22P (8-22) in dorsal root ganglion neurons isolated from transgenic mice expressing human MRGPRX1 when used at a concentration of 5 µM.² Intrathecal administration of ML-382 (5 µl of a 25 µM solution) decreases formalin-induced paw licking and shaking in MRGPRX1 transgenic mice.

WARNING This product is not for human or veterinary use.

1. Wen, W., Wang, Y., Li, Z., et al. Discovery and characterization of 2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide, ML382: A potent and selective positive allosteric modulator of MrgX1. ChemMedChem 10(1), 57-61 (2015).

2. Li, Z., Tseng, P.-Y., Tiwari, V., et al. Targeting human Mas-related G protein-coupled receptor X1 to inhibit persistent pain. Proc. Natl. Acad. Sci. USA 114(10), E1996-E2005 (2017).