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ML382 is a potent and selective MrgX1 (Mas-related G protein-coupled receptor X1, MRGPRX1) positive allosteric modulator with EC50 of 190 nM. ML382 dose-dependently increases the potency of BAM8–22. In vivo, ML382 (5 μM) significantly increases inhibition of ICa by a low concentration of BAM8–22 (0.5 μM) in DRG neurons from MrgprX1 mice. ML382 enhances the inhibition of spinal synaptic transmission by BAM8-22 in MrgprX1 mice. ML382 (25 μM, 125 μM, and 250 μM; 5 μL; i.th.;) dose-dependently attenuates heat hypersensitivity in MrgprX1 mice. ML382 (lumbar puncture injection; 25 μM, 5 μL) leads to a significant increase in postconditioning time spent in the ML382-paired chamber, compared with the preconditioning value. ML382 inhibits nerve injury-induced ongoing pain in MrgprX1 mice.
| Molecular Weight | 360.43 |
| Formula | C18H20N2O4S |
| CAS Number | 1646499-97-9 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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