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-110285
    ML382
    		99.89%
    ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM.
    ML382
  • HY-115682
    (S)-ZINC-3573
    		99.89%
    (S)-ZINC-3573 is an inactive enantiomer of ZINC-3573. (R)-ZINC-3573 is a selective MRGPRX2 agonist. (S)-ZINC-3573 and (R)-ZINC3573 are effective and internally controlled probe-pairs for investigating the biology of primate-exclusive receptor.
    (S)-ZINC-3573
  • HY-145893
    MrgprX2 antagonist-7
    		Antagonist
    MrgprX2 antagonist-7 (compound 10) is an anti-allergic agent. MrgprX2 antagonist-7 shows excellent anti-allergy effects and can inhibit mast cell degranulation.
    MrgprX2 antagonist-7
  • HY-145892
    MrgprX2 antagonist-6
    		Antagonist
    MrgprX2 antagonist-6 (compound 9) is an anti-allergic agent. MrgprX2 antagonist-6 shows excellent anti-allergy effects and can inhibit mast cell degranulation.
    MrgprX2 antagonist-6
  • HY-155480
    PSB-22034
    		Agonist
    PSB-22034 (compound 30d) is a selective agonist of MRGPRX4 with EC50s of 11.2 nM and 30.0 nM in Ca2+ and β-arrestin experiments, respectively.
    PSB-22034
  • HY-P3419A
    PAMP-12 (unmodified) (TFA)
    		Agonist
    PAMP-12 (unmodified) TFA is a potent MRGPRX2 (MrgX2) agonist (EC50=20-50 nM). PAMP-12 (unmodified) is an endogenous peptide that elicit hypotension through inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells.
    PAMP-12 (unmodified) (TFA)
  • HY-122967
    Isosalvianolic acid C
    		Activator
    Isosalvianolic acid C is a phenolic compound that can be found in Lavandula angustifolia Mill.. Isosalvianolic acid C can be used as antioxidant.
    Isosalvianolic acid C
  • HY-148492
    Mrgx2 antagonist-2
    		Antagonist
    Mrgx2 antagonist-2 is a Mrgx2 antagonist (Example 123 in reference patent) with a pIC50 of 8.6. Mrgx2 antagonist-2 can be used in the research of MrgX2 -mediated diseases or disorders.
    Mrgx2 antagonist-2
  • HY-143880
    MRGPRX1 agonist 4
    		Agonist
    MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain.
    MRGPRX1 agonist 4
  • HY-P3843
    Neuropeptide AF (cattle)
    		Agonist
    Neuropeptide AF (cattle), an amidated octadecapeptide, is RFamide neuropeptide. Neuropeptide AF (cattle) acts as a ligand of Mas-related gene receptor A4 (MrgprA4) (Mas-related G-protein-coupled Receptor (MRGPR)) (EC50 of ~60 nM) and MrgprC11 (EC50 of ~300 nM). Neuropeptide AF (cattle) also activate to the G protein-coupled receptors NPFF1 (Neuropeptide Y Receptor) (EC50 of ~25-325 nM) and NPFF2 (EC50 of ~1-5 nM). Neuropeptide AF (cattle) shows anti-opiate and related pain modulation effects.
    Neuropeptide AF (cattle)
  • 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-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-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-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-W354369
    1-(4-Fluorobenzyl)-1H-indazole-3-carboxylic acid
    		Antagonist
    1-(4-Fluorobenzyl)-1H-indazole-3-carboxylic acid (Compound 31) is a metabolite of AB-FUBINACA. 1-(4-Fluorobenzyl)-1H-indazole-3-carboxylic acid is a MRGPRX4 antagonist (IC50: >2.5 μM).
    1-(4-Fluorobenzyl)-1H-indazole-3-carboxylic acid
  • 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-172458
    Z-3578
    		Inhibitor
    Z-3578 is a small-molecule antagonist targeting MrgX2 (Mas-related G protein-coupled receptor X2) with significant anti-pseudoallergic activity and a KD value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppressing the release of β-hexosaminidase with IC50 values of 4.90 µM and 6.18 µM, respectively. It also markedly reduces the release of histamine and TNF-α, along with intracellular calcium flux. In a murine pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation and lowers serum histamine levels, indicating potent in vivo anti-allergic effects. Z-3578 holds promise as a lead compound for the treatment of allergic diseases, especially pseudoallergic reactions.
    Z-3578
Cat. No. Product Name / Synonyms Application Reactivity