MRGPR

MrgprX2 antagonist-8 is an MrgprX2 antagonist that can be used to study inflammatory diseases.

(R)-ZINC-3573 is a potent and highly selective MRGPRX2 probe that activates endogenous MRGPRX2 in a human mast cell line, inducing degranulation and calcium release.

MRGPRX1 agonist 1 is a highly potent agonist of MRGPRX1 (Mas-related G-protein-coupled receptor X1) with an EC50 of 50 nM.

MRGPRX4 modulator-2 (compound 1-55) is a highly potent antagonist of MRGPRX4 with an IC50 value of less than 100 nM. Its notable applications include research on autoimmune diseases such as psoriasis, multiple sclerosis, Steven Johnson's Syndrome, and various chronic itch conditions [1].

ML382 is a potent and selective MrgX1 positive allosteric modulator (EC50 : 190 nM).

BAM (8-22) acetate is a proteolytically cleaved product of proenkephalin A. BAM (8-22) acetate activates Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1, and induces scratching in mice in an Mrgpr-dependent manner.

(S)-ZINC 3573 is a negative control for (R)-ZINC 3573. (S)-ZINC 3573 displays no activity at MRGPRX2 at concentrations below 100 μM.

MrgprX2 antagonist-5, which acts as a potent antagonist of MrgprX2. It exhibits the ability to effectively inhibit the activity of MrgprX2, making it an ideal candidate for research related to inflammatory skin disorders.

MrgprX2 antagonist-4 and compound B-51 E117, is a potent MrgprX2 antagonist. It specifically targets and inhibits the MrgprX2 receptor, making it suitable for investigating various inflammatory skin disorders.

PAMP-12 (unmodified), an endogenous peptide and potent MRGPRX2 (MrgX2) agonist (EC50=20-50 nM), induces hypotension by inhibiting catecholamine release from sympathetic nerve endings and adrenal chromaffin cells [1].

MRGPRX4 modulator-1 (compound 31-2) is a potent antagonist of the mas-related G-protein receptor X4 (MRGPR X4) with an IC50 < 100 nM against MRGPR4, utilized for investigating MRGPR X4-dependent diseases including itch, pain, and autoimmune disorders [1].

MS47134, a selective and potent MRGPRX4 agonist, exhibits an EC50 of 149 nM and holds potential for researching pain, itch, and mast cell-mediated hypersensitivity.

MrgprX2 antagonist-7 is an anti-allergic agent with significant anti-allergic effects and inhibits mast cell degranulation.

MRGPRX2 modulator-1 (example 17), a modulator of the mas-related G-protein receptor X2 (MRGPRX2), is employed in studies focused on inflammation, pain, and autoimmune disorders [1].

Z-3578 is a small molecule antagonist targeting the MrgX2 (Mas-related G protein-coupled receptor X2) with notable anti-pseudoallergic properties, exhibiting a KD value of 729 nM. It effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, with IC50 values of 4.90 µM and 6.18 µM, respectively, suppresses the release of β-hexosaminidase, and significantly reduces the release of histamine and TNF-α, as well as intracellular calcium flux. Additionally, in a mouse pseudoallergy model, Z-3578 significantly alleviates foot swelling, dye leakage, and reduces serum histamine levels, indicating a strong in vivo anti-allergic effect. Z-3578 presents as a promising lead compound in the field of anti-allergic treatments, particularly for pseudoallergic reactions.

PAMP-12 (unmodified) TFA, an endogenous peptide and potent MRGPRX2 (MrgX2) agonist (EC50=20-50 nM), induces hypotension by inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells [1].

MrgprX2 antagonist-6 is a potent antiallergic agent with inhibitory effects on mast cell degranulation.

MRGPRX1 agonist 4 is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive conformation modulator (EC50: 0.1 μM). MRGPRX1 agonist 4 ameliorated the behavioral thermal allergic response in mice, a model of MRGPRX1 neuropathic pain.

BAM(8-22) TFA, a proteolytically cleaved fragment of proenkephalin A, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), specifically MrgprC11 and hMrgprX1, inducing scratching in mice via an Mrgpr-dependent pathway [1].

Setomagpran is an antagonist of the mas-related G protein-coupled receptor (MRGPR) and possesses anti-inflammatory properties.

EP-3945 is an agonist of Mas-related G protein-coupled receptors (MRGPR), exhibiting greater potency than the small molecule agonist β-Alanine targeting MRGPRD. MRGPRs play a crucial role in inflammatory itch and pain perception. These receptors interact with Gq (MRGPRX2, MRGPRX4, and MRGPRX1 are coupled with Gq; MRGPRX2 and MRGPRD couple with Gi), with EP-3945 having an EC50 value of 211.6 nM for Gq.

Mrgx2 antagonist-3 (Compound B-40) is a highly selective antagonist of the MrgX2 receptor, with an IC50 range of 0.042-2.5 nM. It blocks downstream G protein signaling and β-arrestin recruitment, inhibiting Mrgx2 receptor-mediated calcium influx and cell degranulation. Mrgx2 antagonist-3 shows potential for research in inflammation-associated diseases and pruritus, such as chronic urticaria and allergic asthma.

MrgprX2 antagonist-3 is a potent inhibitor of MrgprX2. It holds promising potential for investigating skin inflammatory disorders.

MRGPRX1 agonist 2 (compound 1a) is a potent positive allosteric modulator of Mas-related G protein-coupled receptor X1 (MRGPRX1) with an EC50 value of 0.48 μM, and has potential for use in neuropathic pain research [1].