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ML382

Cat. No. M10642
ML382 Structure
Synonym:

ML-382

Size Price Availability
10mM*1mL in DMSO USD 150  USD150 4-7 Days
10mg USD 140  USD140 4-7 Days
25mg USD 300  USD300 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 360.43
Formula C18H20N2O4S
CAS Number 1646499-97-9
Purity >98.5%
Solubility DMSO ≥ 90 mg/mL
Storage at -20°C
References

[1] Zhe Li, et al. Proc Natl Acad Sci U S A . Targeting human Mas-related G protein-coupled receptor X1 to inhibit persistent pain

[2] Wandong Wen, et al. ChemMedChem . Discovery and characterization of 2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide, ML382: a potent and selective positive allosteric modulator of MrgX1

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  Catalog
Abmole Inhibitor Catalog 2017




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