Cayman Ml-382; 50 Mg; 1646499-97-9; ≥98%

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 (25 µM/animal) decreases formalin-induced paw licking and shaking in MRGPRX1 transgenic mice.

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