Mas-related G-protein-coupled Receptor (MRGPR) Modulator

MRGPRX2 modulator-1 (example 17) is a mas-related g-protein receptor x2 (MRGPRX2) modulator. MRGPRX2 modulator-1 can be used for the research of inflammation, pain and autoimmune disorders.

MRGPRX2 modulator-3 (Compound 4-400) is a quinoline derivative and a MRGPRX2 modulator. MRGPRX2 modulator-3 can be used in the research of MRGPRX2-related diseases, such as allergies, pruritus, pain, inflammation and autoimmune diseases, etc.

BCFTP is a potent, orally active and selective human Mas-related G protein-coupled receptor X1 (MrgprX1)-positive allosteric modulator. BCFTP selectively potentiates MrgprX1 signaling in HEK293 cells. BCFTP alleviates specific neuropathic pain-related behaviors in a humanized MrgprX1 mouse model of chronic constrictive injury (CCI) in a MrgprX1-dependent manner. BCFTP synergistically enhances psychoactive substances analgesia in CCI MrgprX1 mice. BCFTP can be used for neuropathic pain research.

MRGPRX4 modulator-3 (Compound 1C) is a negative allosteric MAS-related G-protein-coupled receptor X4 (MRGPRX4) modulator. MRGPRX4 modulator-3 significantly attenuates Nateglinide (HY-B0422) (orthosteric agonist)-induced responses with an IC₅₀ of 337 nM. MRGPRX4 modulator-3 can be used for chronic itch (especially cholestatic itch) and pain research.