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).

Mas-related G-protein-coupled Receptor (MRGPR) Related Products (14):

Cat. No. Product Name Effect Purity
  • 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.
  • HY-130118
    MRGPRX1 agonist 1
    		99.97%
    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.
  • HY-P1241
    BAM(8-22)
    		99.91%
    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.
  • HY-110285
    ML382
    		98.86%
    ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM.
  • 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.
  • 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.
  • 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.
  • 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.
  • HY-145195
    MrgprX2 antagonist-5
    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.
  • HY-145192
    MrgprX2 antagonist-2
    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.
  • 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.
  • HY-145193
    MrgprX2 antagonist-3
    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.
  • HY-145194
    MrgprX2 antagonist-4
    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.
  • HY-P1241A
    BAM(8-22) TFA
    BAM(8-22) TFA, 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.