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MRGPRX1 inhibitor 1t

Chemical Structure : MRGPRX1 inhibitor 1t

CAS No.: 2764889-60-1

MRGPRX1 inhibitor 1t

Catalog No.: PC-72741Not For Human Use, Lab Use Only.

MRGPRX1 inhibitor 1t is a potent, selective, positive allosteric modulator (PAM) of Mas-related G protein-coupled receptor X1 (MRGPRX1) with EC50 of 0.1 uM.

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    Biological Activity

    MRGPRX1 inhibitor 1t is a potent, selective, positive allosteric modulator (PAM) of Mas-related G protein-coupled receptor X1 (MRGPRX1) with EC50 of 0.1 uM.
    MRGPRX1 inhibitor 1t can be distributed to the spinal cord, the presumed site of action, following oral administration.
    In a neuropathic pain model induced by sciatic nerve chronic constriction injury (CCI), compound 1t (100 mg/kg, po) reduced behavioral heat hypersensitivity in humanized MRGPRX1 mice.
    Mas-related G protein-coupled receptor X1 (MRGPRX1) is a human sensory neuron-specific receptor and potential target for the treatment of pain.

    Physicochemical Properties

    M.Wt 513.356
    Formula C23H17Cl2F3N2O2S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    6-(tert-butyl)-5-(3,4-dichlorophenyl)-4-(2-(trifluoromethoxy)phenoxy)thieno[2,3-d]pyrimidine

    References

    1. Ilyas Berhane, et al. J. Med. Chem. 2022

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