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5 Results for "

MRGPRB2

" in MedChemExpress (MCE) Product Catalog:

Products (5)

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CCG258747

1 Cited Publications

Cat. No.: HY-139690

CAS No.: 2615910-00-2

Purity: 98.96%

Target:

Opioid Receptor G Protein-coupled Receptor Kinase (GRK) Mas-related G-protein-coupled Receptor (MRGPR)

Research Areas:

Cardiovascular Disease Inflammation/Immunology

CCG258747 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) ^[2].

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PSB-172656

Cat. No.: HY-176446

CAS No.: 2641397-91-1

Target:

Research Areas:

Inflammation/Immunology

PSB-172656 is a selective MRGPRX2 antagonist with a K_i of 0.142 nM. PSB-172656 competitively blocks receptor activation by multiple agonists, inhibits Gαq/Gαi dissociation and β-arrestin recruitment, and blocks CXCL14-induced MRGPRX2 calcium mobilization and MRGPRB2 activation. PSB-172656 blocks signaling of the mouse ortholog and mast cell activation, and prevents agonist-induced tracheal contraction, hind paw edema, and systemic anaphylactic symptoms. PSB-172656 can be used for research on mast cell-mediated hypersensitivity and chronic inflammatory diseases .

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GE1111

Cat. No.: HY-158990

CAS No.: 2883669-12-1

Target:

Research Areas:

Inflammation/Immunology

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 ^[2] .

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