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-145191
    MrgprX2 antagonist-1
    		99.93%
    MrgprX2 antagonist-1 is an MrgprX2 antagonist extracted from patent WO2021092264A1, example E23. MrgprX2 antagonist-1 can be used for the research of inflammatory disorders of the skin.
    MrgprX2 antagonist-1
  • HY-P1241
    BAM(8-22)
    		99.95%
    BAM(8-22), a proteolytically cleaved product of proenkephalin A, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1, and induces scratching in mice in an Mrgpr-dependent manner.
    BAM(8-22)
  • HY-146220
    MrgprX2 antagonist-8
    		Antagonist
    MrgprX2 antagonist-8 (example 5b) is a MrgprX2 antagonist. MrgprX2 antagonist-8 can be used for the research of inflammatory disorders.
    MrgprX2 antagonist-8
  • HY-148244
    MS47134
    		99.88%
    MS47134 is a potent and selective MRGPRX4 agonist with an EC50 value of 149 nM. MS47134 can be used for research of pain, itch and mast cell-mediated hypersensitivity.
    MS47134
  • HY-118069
    (R)-ZINC-3573
    		Agonist 99.81%
    (R)-ZINC-3573 is a selective Mas-related G protein-coupled receptor X2 (MRGPRX2) agonist with an EC50 value of 740 nM. (R)-ZINC-3573 can be used as a MRGPRX2 probe for the research of pain and itch.
    (R)-ZINC-3573
  • HY-156830A
    (4′R)-TGR5 Receptor Agonist 4
    		Control
    (4′R)-TGR5 Receptor Agonist 4 is the R enantiomer of TGR5 Receptor Agonist 4 (HY-156830). TGR5 Receptor Agonist 4 is an agonist of Bile Acid Receptor (TGR5), with EC50 for hTGR5 and mTGR5 of 2 nM and 3 nM, respectively. TGR5 Receptor Agonist 4 plays important roles in hypoglycemic and weight loss.
    (4′R)-TGR5 Receptor Agonist 4
  • 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-P3419
    PAMP-12 (unmodified)
    		99.30%
    PAMP-12 (unmodified) 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)
  • HY-147051
    MRGPRX4 modulator-2
    		99.64%
    MRGPRX4 modulator-2 (compound 1-55) is a potent MRGPR X4 modulator, possessing antagonist activity against MRGPR X4 with an IC50 < 100 nM. MRGPRX4 modulator-2 can be used for researching autoimmune diseases such as psoriasis, multiple sclerosis, Steven Johnson’s Syndrome, and other chronic itch conditions.
    MRGPRX4 modulator-2
  • HY-130118
    MRGPRX1 agonist 1
    		99.95%
    MRGPRX1 agonist 1 is a highly potent agonist of MRGPRX1 (Mas-related G-protein-coupled receptor X1), with an EC50 of 50 nM, and is inactive on MRGPRC11. Analgesic effect.
    MRGPRX1 agonist 1
  • HY-145997
    MRGPRX4 modulator-1
    		99.09%
    MRGPRX4 modulator-1 (compound 31-2) is a potent mas-related g-protein receptor X4 (MRGPR X4) modulator, with antagonist activity of IC50 < 100 nM for MRGPR4. MRGPRX4 modulator-1 can be used for researching MRGPR X4 dependent diseases such as itch, pain, and autoimmune disorders.
    MRGPRX4 modulator-1
  • HY-145193
    MrgprX2 antagonist-3
    		99.73%
    MrgprX2 antagonist-3 is an MrgprX2 antagonist extracted from patent WO2021092240A1, example E117. MrgprX2 antagonist-3 can be used for the research of inflammatory disorders of the skin.
    MrgprX2 antagonist-3
  • HY-145192
    MrgprX2 antagonist-2
    		99.20%
    MrgprX2 antagonist-2 is an MrgprX2 antagonist extracted from patent WO2021092262A1, example E163. MrgprX2 antagonist-2 can be used for the research of inflammatory disorders of the skin.
    MrgprX2 antagonist-2
  • HY-156907
    ZINC49534341
    		Antagonist 99.13%
    ZINC49534341 is a MRGPRX2 antagonist, with a Ki of 32 nM.
    ZINC49534341
  • HY-145195
    MrgprX2 antagonist-5
    		≥98.0%
    MrgprX2 antagonist-5 is an MrgprX2 antagonist extracted from patent WO2020223255A1, example 16. MrgprX2 antagonist-5 can be used for the research of inflammatory disorders of the skin.
    MrgprX2 antagonist-5
  • 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-145194
    MrgprX2 antagonist-4
    		99.85%
    MrgprX2 antagonist-4 is an MrgprX2 antagonist extracted from patent US20210128561A1, compound B-51 E117. MrgprX2 antagonist-4 can be used for the research of inflammatory disorders of the skin.
    MrgprX2 antagonist-4
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity