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).
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Mas-related G-protein-coupled Receptor (MRGPR) Inhibitors
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Mas-related G-protein-coupled Receptor (MRGPR) Agonists
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Mas-related G-protein-coupled Receptor (MRGPR) Antagonists
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Mas-related G-protein-coupled Receptor (MRGPR) Activators
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Mas-related G-protein-coupled Receptor (MRGPR) Modulators
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Mas-related G-protein-coupled Receptor (MRGPR) Related Products (61)
Related Products (61)
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Antibodies (1)
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MrgprX2 antagonist-1
0 ImagesMrgprX2 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.
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PAMP-12 (unmodified)
0 ImagesPAMP-12 (unmodified) is an endogenous peptide and is a MrgX2 agonist. PAMP-12 (unmodified) can reduce cAMP accumulation, increase Ca2+ levels, enhance beta-arrestin recruitment, decrease IP-1, and increases phosphoERK. PAMP-12 (unmodified) can elicit hypotension through inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells. PAMP-12 (unmodified) can be used for the research of hypotension and ulcerative colitis.
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BAM(8-22)
0 ImagesBAM(8-22), 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) induces scratching in mice in an Mrgpr-dependent manner. In addition, BAM(8-22) has an analgesic effect and can also inhibit the activation of microglia.
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MrgprX2 antagonist-8
0 ImagesCat. No.: HY-146220CAS No.: 2768216-96-0MrgprX2 antagonist-8 (example 5b) is a MrgprX2 antagonist. MrgprX2 antagonist-8 can be used for the research of inflammatory disorders.
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MrgprX2 antagonist-2
0 ImagesMrgprX2 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.
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MrgprX2 antagonist-10
0 ImagesMrgprX2 antagonist-10 is a potent MRGPRX2 antagonist. MrgprX2 antagonist-10 inhibits MRGPRX2-mediated accumulation and mast cell degranulation (IC50 < 100 nM), thereby blocking mast cell activation. MrgprX2 antagonist-10 can be used in research on MRGPRX2-related inflammatory and allergic diseases.
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MrgprX2 antagonist-11
0 ImagesMrgprX2 antagonist-11 is a potent MrgprX2 antagonist. MrgprX2 antagonist-11 inhibits MrgprX2-mediated accumulation and mast cell degranulation (IC50 < 100 nM), thereby blocking mast cell activation. MrgprX2 antagonist-11 can be used in research on MrgprX2-related inflammatory and allergic diseases.
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HEP-50768
0 ImagesHEP-50768 is an orally active and selective MRGPRX4 (hX4) antagonist. HEP-50768 suppresses basal and bile-acid-stimulated hX4 activity. HEP-50768 binds the receptor’s transmembrane pocket and induces extracellular loop rearrangements. HEP-50768 modulates GPCR microswitch motifs and reduces bile-acid-induced pruritic scratching behaviors. HEP-50768 can be used for the research of cholestatic pruritus.
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MrgprX2 antagonist-3
0 ImagesMrgprX2 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.
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(R)-ZINC-3573
0 Images(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.
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PAMP-12(human, porcine)
0 ImagesCat. No.: HY-P2198CAS No.: 196305-05-2PAMP-12(human, porcine) is a major component of immunoreactive (ir)-PAMP, is processed from the adrenomedullin precursor, is a potent hypotensive peptide and participates in cardiovascular control.
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Nelremagpran
0 ImagesSynonyms: MRGPRX4 modulator-2MRGPRX4 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.
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MrgprX2 antagonist-5
0 ImagesMrgprX2 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.
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MRGPRX4 modulator-1
0 ImagesMRGPRX4 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.
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Mrgx2 antagonist-3
0 ImagesMrgx2 antagonist-3 (Compound B-40) is a highly selective antagonist of MrgX2 receptor with an IC50 value of 0.042-2.5 nM. Mrgx2 antagonist-3 blocks downstream G protein signaling and β-Arrestin recruitment, thereby inhibiting MrgX2 receptor-mediated calcium influx and cellular degranulation. Mrgx2 antagonist-3 is promising for research of inflammation-related diseases and pruritus, such as chronic urticaria, allergic asthma.
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MRGPRX1 agonist 1
0 ImagesMRGPRX1 agonist 1 is a highly potent MRGPRX1 agonist (EC50=50 nM) with greater than 50-fold selectivity for δ, μ, and κ opioid receptors. MRGPRX1 agonist 1 is inactive against MRGPRC11. MRGPRC11 inhibits high voltage-activated (HVA) Ca2+ currents, reduces neurotransmitter release, and mitigates nociceptive transmission in the spinal cord. MRGPRX1 agonist 1 is useful for the study of chronic pain, especially neuropathic pain.
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CCG258747
0 ImagesCCG258747 is a selective GRK2 inhibitor (IC50 = 18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, > 5500, and > 550-fold, respectively). CCG258747 also blocks the internalization of the µ-opioid receptor (MOR). CCG258747 attenuates IgE mediated anaphylaxis by inhibiting GRK2 and FcεRI signaling pathway but activates mast cells via MRGPRX2 and MRGPRB2. CCG258747 can be used to study diseases related to overexpression of GRK2 (such as heart failure, opioid tolerance).
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Imidazolidinyl urea
0 ImagesImidazolidinyl 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.
