2. Signaling Pathways
  3. GPCR/G Protein
  4. Mas-related G-protein-coupled Receptor (MRGPR)

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

Mas-related G-protein-coupled Receptor (MRGPR) is a novel family of sensory nerve specific orphan G protein coupled receptors (GPCRs). This family was characterized more than 30 years ago with the description of the Mas gene encoding for oncogene-like MAS receptors. The MRGPR family that now gathers more than 50 members in rodents and humans. On the basis of sequence homology, the family of MRGPRs can be divided into several subfamilies, namely, MRGPRA to MRGPRG and MRGPRX. Of these, the subfamilies MRGPR-A, MRGPR-B, and MRGPR-C are uniquely conserved in rodents, whereas the subfamily MRGPRX is characteristic among primates and humans. In humans, 4 MRGPRX genes, MRGPRX1, MRGPRX2, MRGPRX3, and MRGPRX4, have been described.

MRGPRs were first identified on specialized sensory neurons that encode itch (pruriceptors) and pain (nociceptors). Importantly, activation of Mrgprs expressed at the surface of sensory neurons has been shown to induce both itch and pain sensations. Most MRGPRs are associated with nociception and itch transmission, through their binding to various itch-inducing or painassociated substances: such as β–alanine, chloroquine (CQ), or substance P (SP).

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-147106
    Mrgx2 antagonist-1
    		Antagonist
    Mrgx2 antagonist-1 (example 1) is a potent Mrgx2 (Mas-related Gene X2) antagonist. Mrgx2 antagonist-1 can be used for the research of MrgX2-mediated diseases and disorders.
    Mrgx2 antagonist-1
  • HY-179458
    JHU-58
    		Agonist
    JHU-58 is a peptidomimetic agonist targeting mouse MRGPRC11 and rat MRGPRC receptors. JHU-58 demonstrates analgesic effects in mouse models of neuropathic pain. JHU-58 is promising for research of neuropathic pain.
    JHU-58
  • HY-P11478
    Catestatin (mouse)
    		Inhibitor
    Catestatin (mouse) is an antimicrobial peptide. Catestatin (mouse) robustly activates Mrgprb2 with an EC50 of 59.73 μM. Catestatin (mouse) is effective in promoting MRSA clearance from wound infections. Catestatin (mouse) dampens the inflammatory immune response to MRSA infection.
    Catestatin (mouse)
  • HY-184281
    XAT-14
    XAT-14 is a Furanocoumarin derivative. XAT-14 competes with agonists to bind to the active pocket of MRGPRX2, inhibiting calcium influx and mast cell degranulation. XAT-14 suppresses the release of histamine, IL-8 and MCP-1 induced by Compound 48/80 (HY-115768). XAT-14 inhibits local allergic inflammation. XAT-14 can be used for the research of pseudo-allergic diseases.
    XAT-14
  • HY-143878
    MRGPRX1 agonist 2
    		Agonist
    MRGPRX1 agonist 2 (compound 1a) is a potent Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.48 μM. MRGPRX1 agonist 2 can be used for researching neuropathic pain.
    MRGPRX1 agonist 2
  • HY-175672
    MRGPRX4 modulator-3
    		Modulator
    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.
    MRGPRX4 modulator-3
  • HY-176767
    MrgprX2-IN-1
    		Antagonist
    MrgprX2-IN-1 (Compound 2-10) is a selective Mas-related G-protein coupled receptor X2 (MRGPRX2) antagonist. MrgprX2-IN-1 blocks IgE-independent immune responses by inhibiting MRGPRX2-mediated mast cell degranulation and release of inflammatory mediators. MrgprX2-IN-1 is promising for research of pseudo-allergic reactions, chronic pruritus, and inflammatory diseases.
    MrgprX2-IN-1
  • HY-173004A
    (Rac)-EP-2825
    		Agonist
    (Rac)-EP-2825 (Compound 8-6) is a MRGPRD agonist with an IC50 value between 100 and 500 nM. (R)-EP-2825 can be used in the research of pain.
    (Rac)-EP-2825
  • HY-P2198A
    PAMP-12(human, porcine) TFA
    		Agonist
    PAMP-12(human, porcine) TFA is a major component of immunoreactive (ir)-PAMP, is processed from the adrenomedullin precursor, is a potent hypotensive peptide and participates in cardiovascular control.
    PAMP-12(human, porcine) TFA
  • HY-P1241A
    BAM(8-22) TFA
    BAM(8-22) TFA, a proteolytically cleaved product of proenkephalin A and sensory neuron-specific receptor (SNSR) agonist, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1. BAM(8-22) TFA induces scratching in mice in an Mrgpr-dependent manner. In addition, BAM(8-22) TFA has an analgesic effect and can also inhibit the activation of microglia.
    BAM(8-22) TFA
  • HY-181891
    XAT-13
    XAT-13 is an orally active antiallergic agent. XAT-13 binds to the active pocket of MRGPRX2, and inhibits C48/80-induced calcium influx and β-hexosaminidase release. XAT-13 can be used for the research of pseudo-allergic diseases.
    XAT-13
  • HY-176768
    MrgprX2-IN-2
    		Antagonist
    MrgprX2-IN-2 (Compound example 12) is a selective Mas-related G-protein coupled receptor X2 (MRGPRX2) antagonist. MrgprX2-IN-2 blocks IgE-independent immune responses by inhibiting MRGPRX2-mediated mast cell degranulation and release of inflammatory mediators. MrgprX2-IN-2 is promising for research of pseudo-allergic reactions, chronic pruritus, and inflammatory diseases.
    MrgprX2-IN-2
  • HY-143879
    MRGPRX1 agonist 3
    		Agonist
    MRGPRX1 agonist 3 (compound 1f) is a potent Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.22 μM. MRGPRX1 agonist 3 can be used for researching neuropathic pain.
    MRGPRX1 agonist 3
  • HY-172438
    Setomagpran
    		Antagonist
    Setomagpran is the antagonist for mas-related G protein-coupled receptor (MRGPR), and exhibits anti-inflammatory activity.
    Setomagpran
  • HY-145193A
    (R)-MrgprX2 antagonist-3
    		Antagonist
    (R)-MrgprX2 antagonist-3 (compound E118) is an MrgprX2 antagonist extracted from patent WO2021092240A1, example E118. (R)-MrgprX2 antagonist-3 can be used for the research of inflammatory disorders of the skin.
    (R)-MrgprX2 antagonist-3
  • HY-111273
    AR244555
    		Antagonist
    AR244555 is a malate-aspartate shuttle (MAS) inverse agonist with IC50s of 186 nM and 348 nM in human and rat inositol phosphatase (IP) Gq coupling assays respectively. AR244555 has cardioprotective effects.
    AR244555
  • HY-B1158R
    Imidazolidinyl urea (Standard)
    		Activator
    Imidazolidinyl urea (Standard) is the analytical standard of Imidazolidinyl urea. This product is intended for research and analytical applications. Imidazolidinyl urea is a commonly used antibacterial preservative in cosmetics and pharmaceuticals that releases formaldehyde through decomposition. Imidazolidinyl urea can also be used in the preparation of multifunctional hydrogels for the care of infectious wounds. Imidazolidinyl urea has broad-spectrum antibacterial activity, which mainly inhibits the reproduction of gram-negative bacteria and gram-positive bacteria, and restricts the growth of yeast and mold to a certain extent. Imidazolidinyl urea can induce non-histaminergic allergy by MRGPRX2 activation of mast cells.
    Imidazolidinyl urea (Standard)
  • HY-W242735
    4-Aminobenzimidamide Hydrochloride
    		Agonist
    4-Aminobenzimidamide Hydrochloride (Compound 4a) is a MRGPRX1 agonist. 4-Aminobenzimidamide Hydrochloride can be used in the study of MRGPRX1-mediated analgesic effects.
    4-Aminobenzimidamide Hydrochloride
  • HY-183945
    WO-459
    		Agonist
    WO-459 is a potent Gpr52 agonist. WO-459 induces dose-dependent elevation of intracellular cAMP in cells expressing Gpr52. WO-459 can be used for the research of Huntington’s disease and psychotic disorders.
    WO-459
  • HY-156073
    LY3325656
    		Agonist
    LY3325656 is a selective GPR142 agonist. LY3325656 selectively activates GPR142. LY increases glucose-dependent insulin secretion. LY3325656 shows anti-diabetic effects. LY3325656 can be used in the research of type 2 diabetes.
    LY3325656
Cat. No. Product Name / Synonyms Application Reactivity