ML-382

ML-382 is a positive allosteric modulator of MAS-related G protein-coupled receptor family member X1 (MRGPRX1). It potentiates activation of MRGPRX1 induced by the MRGPRX1 agonist BAM 22P (8-22) (Cay-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 (ICa ) 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. Intrathecal administration of ML-382 (25 µM/animal) decreases formalin-induced paw licking and shaking in MRGPRX1 transgenic mice.Formal Name: 2-[(cyclopropylsulfonyl)amino]-N-(2-ethoxyphenyl)-benzamide. CAS Number: 1646499-97-9. Synonyms: VU0485891. Molecular Formula: C18H20N2O4S. Formula Weight: 360.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 5 mg/ml, DMSO: 2 mg/ml, Ethanol: 3 mg/ml, PBS (pH 7.2): insol. SMILES: O=S(NC1=C(C=CC=C1)C(NC2=CC=CC=C2OCC)=O)(C3CC3)=O. InChi Code: InChI=1S/C18H20N2O4S/c1-2-24-17-10-6-5-9-16(17)19-18(21)14-7-3-4-8-15(14)20-25(22,23)13-11-12-13/h3-10,13,20H,2,11-12H2,1H3,(H,19,21). InChi Key: RCSLEKLNDJJJLF-UHFFFAOYSA-N.