Name | ML 382 |
Synonyms | ML 382 2-[(Cyclopropylsulfonyl)amino]-N-(2-ethoxyphenyl)benzamide Benzamide, 2-[(cyclopropylsulfonyl)amino]-N-(2-ethoxyphenyl)- |
CAS | 1646499-97-9 |
Molecular Formula | C18H20N2O4S |
Molar Mass | 360.43 |
Density | 1.34±0.1 g/cm3(Predicted) |
Solubility | Soluble in DMSO |
pKa | 8.30±0.20(Predicted) |
Storage Condition | -20°C |
Use | ML382 is a potent selective positive modulator of the Mas-related G protein-coupled receptor X1 MRGPRX1 (MrgX1) with EC50 of 190 nM. |
In vitro study | In the absence of ML382, the IC 50 for BAM8-22 inhibition of I Ca is 0.66 ± 0.05 μM. In the presence of 0.1 μM, 1 μM, 10 μM, and 30 μM ML382, BAM8-22 IC 50 is reduced to 0.43 ± 0.02 μM, 0.25 ± 0.02 μM, 0.06 ± 0.01 μM, and 0.08 ± 0.01 μM, respectively. A lower IC 50 generally indicates a higher potency; thus, ML382 dose-dependently increases the potency of BAM8–22, further demonstrating that ML382 is a positive allosteric modulator of MRGPRX1. |
In vivo study | ML382 (5 μM) significantly increases inhibition of I Ca 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.774 ml | 13.872 ml | 27.745 ml |
5 mM | 0.555 ml | 2.774 ml | 5.549 ml |
10 mM | 0.277 ml | 1.387 ml | 2.774 ml |
5 mM | 0.055 ml | 0.277 ml | 0.555 ml |
biological activity | ML382 is a potent and selective positive regulator of Mas-related G protein-coupled receptor X1 MRGPRX1 (MrgX1), the EC50 was 190 nM. |
Target | EC50: 190 nM (MRGPRX1) |