grpr

GRPR antagonist-1 is a potent antagonist of the gastrin-releasing peptide receptor (GRPR) and displays cytotoxicity to certain cancer cells, including PC3 cells (IC50: 4.97 μM), Pan02 cells (IC50: 4.36 μM), and HGC-27 cells (IC50: 3.40 μM). It reduces Bcl-2 levels, increases Bax levels, inhibits HGC-27 cell viability, and induces apoptosis, thereby exhibiting anti-cancer effects.

GRPR antagonist-2 is a potent antagonist of the gastrin-releasing peptide receptor (GRPR) and exhibits anticancer effects with cytotoxicity to HGC-27 cells (IC50: 0.77 μM) and Pan02 cells (IC50: 2.5 μM).

PD176252 is a potent BB1 and BB2 antagonist with inhibitory effects on BB1 and BB2 receptors.PD176252 acts as a small molecule GRPR inhibitor and FPR1 FPR2 agonist to inhibit the growth and proliferation of a variety of cancer cells.

NOTA-P2-RM26 is a high-affinity NOTA-conjugated bombesin antagonist designed for GRPR-targeted tumor imaging.

BA 1 TFA acts as a potent agonist for the bombesin (BB) family of receptors, exhibiting high affinity binding to Bombesin receptor subtype-3 (BRS3), gastrin-releasing peptide receptor (GRPR), and neuromedin B receptor (NMBR), with IC50 values of 6, 0.4, and 2.5 nM, respectively [1].

[Lys3]-Bombesin is a biologically active peptide used in PET (Positron Emission Tomography) imaging to identify GRPR (gastrin-releasing peptide receptor) positive prostate cancer. The compound, when conjugated with a corresponding monoclonal antibody, can selectively trigger CD64-dependent monocyte and neutrophil-mediated lysis in small cell carcinoma.

PD 168368 is a novel, potent, competitive and selective nonpeptide neuromodulin B receptor (NMB-R) antagonist with inhibitory effects on the gastrin-releasing peptide receptor (GRPR).PD 168368 is a potent mixed agonist of FPR1 FPR2 FPR3.

RC-3095, a selective GRPR antagonist, has been shown to have anti-inflammatory properties in different models of inflammation.

Mammalian bombesin-like peptide neurotransmitter that is an agonist for the gastrin-releasing peptide receptor (GRPR). GRP has been reported to activate GABAergic interneurons in the amygdala leading to increased GABA release and fear suppression in mice

RC-3095 acetate is an antagonist of bombesin gastrin-releasing peptide receptor (GRPR). It exerts protective effects by reducing gastric oxidative injury in the arthritic mice.