antagonist g

Antagonist G is an anticancer peptide and is also a broad spectrum neuropeptide growth factor antagonist.

Antagonist G TFA is a potent antagonist of vasopressin and exhibits weaker antagonistic effects on GRP and Bradykinin. Additionally, this compound promotes AP-1 transcription and enhances cellular sensitivity to chemotherapy [1] [2].

Substance P-related peptide that inhibits binding of G proteins to their receptors. Competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.

GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK/PD characteristics and can be used to study pulmonary fibrosis.

G36 is a cell-permeable non-steroidal antagonist of GPER. G36 inhibits activation by either 17β-estradiol or the GPER-selective agonist G-1 (IC50 = 112 and 165 nM, respectively). G36 has no detectable binding activity to either ERα or ERβ. G36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or G-1 but not by EGF. G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ERα and ERβ in complex biological systems.

UNC0006 is a beta-inhibitory protein biased D(2)R ligand, and is also an antagonist of G(i)-regulated cAMP production and a partial agonist of D(2)R/beta-arrestin-2 interaction. It has antipsychotic activity and is used in the study of neurological disorders.

Dihydromunduletone (DHM) is an adhesion G protein-coupled receptor (aGPCR) antagonist that acts as a chemical probe for the inhibition of GPR56 and GPR114/ADGRG5, which have similar tethered agonists.

SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist, specifically targeting D1 and D5 receptors with Ki values of 0.2 nM and 0.3 nM, respectively.

MA-2029 is selective for the motilin receptor over various other receptors and ion channels. MA-2029 is a selective and competitive motilin receptor antagonist (IC50=4.9 nM). MA-2029 may be useful for gastrointestinal disorders associated with disturbed g

SRX246 has no interaction at V1b and V2 receptors. SRX246 shows negligible binding at 64 other receptors classes, including 35 G-proteincoupled receptors. SRX246 is a potent and CNS-penetrant vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V

Berlafenone (previously known as GK 23 G), is a sodium channel antagonist that has been investigated as a Class Ic antiarrhythmic compound.

PSB-22269 is identified as a GPR17 antagonist with a Ki value of 8.91 nM. It exhibits significant inhibitory effects in cAMP and G protein activation assays. Molecular docking studies indicate that the binding site of PSB-22269 includes positively charged arginine residues and a hydrophobic pocket. PSB-22269 promotes myelin regeneration strategies, offering potential for multiple sclerosis research.

LTD4 antagonist 2 (compound 6) functions as a leukotriene D4 (LTD4) antagonist with an IC50 of 2.8 μM for the cysteinyl leukotriene 1 receptor (CysLT1R). Additionally, it acts as an agonist for the G protein-coupled bile acid receptor 1 (GPBAR1), making it applicable for research into colitis, metabolic syndrome, and other GPBAR1- and CysLT1R-related diseases.

FSH receptor antagonist 1 (compound 10) is a potent antagonist of the G(s) protein-coupled human follicle-stimulating hormone (FSH) receptor. It exhibits an IC50 value of 28 nM in cell lines expressing the human FSH receptor. This compound significantly inhibits follicle growth and ovulation in in vitro mouse models.

GE1111 is an antagonist of the mas-related G protein-coupled receptor X2 (MRGPRX2), exhibiting an IC50 of 9.42 μM. It inhibits mast cell degranulation with an IC50 of 4.7 μM. In the C48/80-induced systemic allergic reaction model, GE1111 demonstrates both antiallergic and anti-inflammatory properties.

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.

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

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.

Amlodipine besilate impurity G is a Calcium Channel antagonist with potential application in the study of neurological diseases and is an impurity in the synthesis of Amlodipine besilate.

NF449 is a potent antagonist of the P2X1 receptor, displaying IC50 values of 0.28 nM, 0.69 nM, and 120 nM for rP2X1, rP2X1+5, and P2X2+3, respectively. It acts selectively against Gsα G proteins (G Protein). NF449 inhibits the binding rate of GTP[γS] to Gsα-s, suppresses the stimulation of adenylate cyclase activity, and blocks the coupling of β-adrenergic receptors with Gs.

GABAB receptor antagonist 4 (Compound 28) is a GABAB receptor antagonist that inhibits GABA-induced G protein activation by competitively binding to the orthosteric site of the GABAB receptor. This compound is useful for researching neurological disorders associated with GABAB receptors.

MrgprX2-IN-1 (Compound 2-10) is a selective antagonist of the Mas-related G protein-coupled receptor X2 (MRGPRX2). It functions by inhibiting mast cell degranulation and the release of inflammatory mediators mediated by MRGPRX2, thereby blocking non-IgE-dependent immune responses. MrgprX2-IN-1 holds potential for research into pseudo-allergic reactions, chronic pruritus, and inflammatory diseases.

GPR15 antagonist-1 (Compound 5) is an agent that inhibits G protein-coupled receptor 15 (GPR15). GPR15 is a well-studied GPCR, associated with conditions such as HIV infection, colitis, and diseases related to smoking.

MrgprX2-IN-2 (Compound example 12) is a selective antagonist of the Mas-related G protein-coupled receptor X2 (MRGPRX2). It works by inhibiting MRGPRX2-mediated mast cell degranulation and the release of inflammatory mediators, thus blocking non-IgE-dependent immune responses. MrgprX2-IN-2 shows potential for research in the areas of pseudo-allergic reactions, chronic pruritus, and inflammatory diseases.