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. 상품명 효과 Purity Chemical Structure
  • HY-160540
    MRGPRX2 modulator-1
    		Modulator 99.03%
    MRGPRX2 modulator-1 (example 17) is a mas-related g-protein receptor x2 (MRGPRX2) modulator. MRGPRX2 modulator-1 can be used for the research of inflammation, pain and autoimmune disorders.
    MRGPRX2 modulator-1
  • HY-145194
    MrgprX2 antagonist-4
    		99.53%
    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-172458
    Z-3578
    		Inhibitor 98.72%
    Z-3578 is an orally active small-molecule antagonist of MrgX2 with potent antipseudoallergic activity, exhibiting a KD value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppresses the release of β-hexosaminidase, significantly reduces the release of histamine and TNF-α, and decreases intracellular calcium flux. In a mouse pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation, and reduces serum histamine levels. Z-3578 can be used for the study of pseudoallergic reactions.
    Z-3578
  • HY-155480
    PSB-22034
    		Agonist 99.61%
    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-P1656
    (D-Pro7)-Angiotensin I/II (1-7)
    		Antagonist 99.95%
    (D-Pro7)-Angiotensin I/II (1-7) is a potent Mas receptor inhibitor with a Ki of 0.001 μM for rat receptors. (D-Pro7)-Angiotensin I/II (1-7) competitively blocks the binding of Angiotensin-(1-7) to the Mas receptor and attenuates the vasodilatory effect of rat aortas under physiological and hypertensive conditions. (D-Pro7)-Angiotensin I/II (1-7) can be used for studies on the function of the renin-angiotensin system and the pathological mechanisms of hypertension.
    (D-Pro7)-Angiotensin I/II (1-7)
  • HY-178793
    MrgprX2 antagonist-9
    		Antagonist 99.92%
    MrgprX2 antagonist-9 is an MRGPRX2 antagonist with an IC50 of 0.1-100 nM. MrgprX2 antagonist-9 can be used for the research of inflammatory diseases.
    MrgprX2 antagonist-9
  • 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-148492
    Mrgx2 antagonist-2
    		Antagonist
    Mrgx2 antagonist-2 (Example 132) is a Mrgx2 antagonist 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-158990
    GE1111
    		Antagonist
    GE1111 is a MRGPRX2 antagonist (IC50 = 9.4 μM). GE1111 inhibits MRGPRX2/MRGPRB2-mediated mast cell activation. GE1111 reduces the expressions of TSLP, IL-13, MCP-1, TNF-α, IL-1β and periostin, maintains the expression levels of claudin 1 and involucrin, restores the phagocytic activity of macrophages, and attenuates the activation of STIM1 and phosphorylated AKT. GE1111 exerts anti-inflammatory and anti-allergic effects in multiple animal models. GE1111 is applicable to the research related to rosacea, atopic dermatitis and ulcerative colitis.
    GE1111
  • HY-174452
    BER-5
    		Antagonist 99.83%
    BER-5 is a potent MrgX2 antagonist. BER-5 possess broad-spectrum antagonistic activity against a diverse range of MrgX2 agonists. BER-5 can inhibit Substance P (SP) (HY-P0201)-induced degranulation of LAD2 cells. BER-5 attenuates SP-induced allergic reactions in mice. BER-5 can be used for the study of allergic reactions.
    BER-5
  • HY-173003
    EP-3945
    		Agonist 99.17%
    EP-3945 is a potent agonist of Mas-related G protein-coupled receptor (MRGPR), more effective than the MRGPRD small molecule agonist β-Alanine (HY-N0230). MRGPR plays a crucial role in inflammatory pruritus and pain sensation. Additionally, MRGPR binds to Gq (MRGPRX2, MRGPRX4, MRGPRX1 couple with Gq; MRGPRX2, MRGPRD couple with Gi), with EP-3945 measured EC50 for Gq being 211.6 nM.
    EP-3945
  • 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-W354369
    1-(4-Fluorobenzyl)-1H-indazole-3-carboxylic acid
    		Antagonist 99.90%
    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-185402
    MrgprX2 antagonist-10
    		Antagonist
    MrgprX2 antagonist-10 (Example 218) is a MrgprX2 antagonist with an IC50 of less than 100 nM. MrgprX2 antagonist-10 can be used for the study of various inflammatory diseases.
    MrgprX2 antagonist-10
  • HY-185405
    MrgprX2 antagonist-11
    		Antagonist
    MrgprX2 antagonist-11 (Example 53) is a MrgprX2 antagonist with an IC50 of less than 100 nM. MrgprX2 antagonist-11 can be used for the study of various inflammatory diseases.
    MrgprX2 antagonist-11
  • HY-164298
    MRGPRX2 modulator-3
    		Modulator
    MRGPRX2 modulator-3 (Compound 4-400) is a quinoline derivative and a MRGPRX2 modulator. MRGPRX2 modulator-3 can be used in the research of MRGPRX2-related diseases, such as allergies, pruritus, pain, inflammation and autoimmune diseases, etc.
    MRGPRX2 modulator-3
  • HY-P3419A
    PAMP-12 (unmodified) TFA
    		Agonist
    PAMP-12 (unmodified) TFA is an endogenous peptide and is a MrgX2 agonist. PAMP-12 (unmodified) TFA can reduce cAMP accumulation, increase Ca2+ levels, enhance beta-arrestin recruitment, decrease IP-1, and increases phosphoERK. PAMP-12 (unmodified) TFA can elicit hypotension through inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells. PAMP-12 (unmodified) TFA can be used for the research of hypotension and ulcerative colitis.
    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-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)
Cat. No. 상품명 / Synonyms Application Reactivity