ML382 | MRGPRX1 positive allosteric modulator

CAS:
 1646499-97-9
Catalog Number:
 10-3937

Available Options

SizePriceQuantity 
10mg$85.00
50mg$300.00

ML382 (1646499-97-9) 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.1  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.2

References/Citations:

  1. Wen, et al. (2015), Discovery and characterization of 2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide, ML382: a potent and selective positive allosteric modulator of MrgX1; ChemMedChem.10 57
  2. Li, et al. (2017), Targeting human Mas-related G protein-coupled receptor X1 to inhibit persistent pain; Proc. Acad. Sci. USA. 114 E1996
CAS:
1646499-97-9
Catalog Number:
10-3937
Activity:
MRGPRX1 positive allosteric modulator
Chemical Names:
2-(Cyclopropanesulfonylamimo)-N-(2-ethoxyphenyl)benzamide
Alternate Name:
VU0485891
Molecular Weight:
360.43
Molecular Formula:

C18H20N2O4S

Solubility:
Soluble in DMSO (>25 mg/ml); Ethanol (5 mg/ml with warming)
Physical Properties:
White solid
Purity:

99% HPLC
NMR (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee