2. Signaling Pathways
  3. GPCR/G Protein
  4. Mas-related G-protein-coupled Receptor (MRGPR)
  5. Mas-related G-protein-coupled Receptor (MRGPR) Antagonist

Mas-related G-protein-coupled Receptor (MRGPR) Antagonist

Mas-related G-protein-coupled Receptor (MRGPR) Antagonists (19):

Cat. No. Product Name Effect Purity
  • 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.
  • HY-183050
    HEP-50768
    		Antagonist
    HEP-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.
  • HY-185727
    MrgprX2 antagonist-12
    		Antagonist
    MrgprX2 antagonist-12 is a human MrgprX2 antagonist with a target pIC50 of 8.7. MrgprX2 antagonist-12 can be used for the research of inflammatory disorders, e.g., inflammatory disorders of the skin.
  • HY-156907
    ZINC49534341
    		Antagonist 99.40%
    ZINC49534341 is a MRGPRX2 antagonist, with a Ki of 32 nM.
  • HY-176446
    Mrgx2 antagonist-3
    		Antagonist 98.24%
    Mrgx2 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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).
  • 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.
  • 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.
  • 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-176767
    MrgprX2-IN-1
    		Antagonist
    MrgprX2-IN-1 (Compound 2-10) is a selective Mas-related G-protein coupled receptor X2 (MRGPRX2) antagonist. MrgprX2-IN-1 blocks IgE-independent immune responses by inhibiting MRGPRX2-mediated mast cell degranulation and release of inflammatory mediators. MrgprX2-IN-1 is promising for research of pseudo-allergic reactions, chronic pruritus, and inflammatory diseases.
  • HY-176768
    MrgprX2-IN-2
    		Antagonist
    MrgprX2-IN-2 (Compound example 12) is a selective Mas-related G-protein coupled receptor X2 (MRGPRX2) antagonist. MrgprX2-IN-2 blocks IgE-independent immune responses by inhibiting MRGPRX2-mediated mast cell degranulation and release of inflammatory mediators. MrgprX2-IN-2 is promising for research of pseudo-allergic reactions, chronic pruritus, and inflammatory diseases.
  • HY-172438
    Setomagpran
    		Antagonist
    Setomagpran is the antagonist for mas-related G protein-coupled receptor (MRGPR), and exhibits anti-inflammatory activity.
  • 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.
  • 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.