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ML382 

Cat. No.: HY-110285
Handling Instructions

ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM.

For research use only. We do not sell to patients.

ML382 Chemical Structure

ML382 Chemical Structure

CAS No. : 1646499-97-9

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Description

ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM[1].

IC50 & Target

EC50: 190 nM (MRGPRX1)[1]

In Vitro

In the absence of ML382, the IC50 for BAM8-22 inhibition of ICa is 0.66 ± 0.05 μM. In the presence of 0.1 μM, 1 μM, 10 μM, and 30 μM ML382, BAM8-22 IC50 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 IC50 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[1].

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[1].

Molecular Weight

360.43

Formula

C₁₈H₂₀N₂O₄S

CAS No.

1646499-97-9

SMILES

O=C(NC1=CC=CC=C1OCC)C2=CC=CC=C2NS(=O)(C3CC3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

ML382ML 382ML-382OtherspainnociceptornervousDRGneuronsinjuryInhibitorinhibitorinhibit

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