ML382, MRGPRX1 positive allosteric modulator

Product Details

Formal Name: 2-(Cyclopropanesulfonylamimo)-N-(2-ethoxyphenyl)benzamide

Alternate Names: VU0485891

Molecular Formula: C₁₈H₂₀N₂O₄S

Formula Weight: 360.5

CAS Number: 1646499-97-9

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (at least 25 mg/ml) or in Ethanol (up to 5 mg/ml, with warming).

Storage: -20°C

Stability: ≥ 2 years.

Applications

MRGPRX1 positive allosteric modulator

Functions

ML382 is a potent (EC₅₀ = 190 nM in the presence of the endogenous peptide MRGX1 agonist BAM8-22) and selective positive allosteric modulator of the Mas-related G protein-coupled receptor X1 (MRGX1 or MRGPRX1), a receptor whose expression is limited to subsets of small-diameter sensory neurons in dorsal root ganglia and trigeminal neurons.  ML382 significantly enhanced the antihyperalgesic effects of exogenously added BAM8-22 and in mouse models of persistent pain without exogenous BAM8-22, suggesting enhanced pain inhibition from a sufficient supply of endogenous MRGPRX1 ligands and a potential new pain therapeutic.

Application Procedures

First dissolved in DMSO (25 mg/ml) or in Ethanol (5 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)