- Signalwege
- GPCR/G Protein
- Bombesin Receptor
Bombesin Receptor
The bombesin (Bn) receptor family includes the gastrin-releasing peptide (GRPR) and neuromedin B (NMBR) receptors, Bn receptor subtype 3 (BRS-3) and Bn receptor subtype 4 (BB4). Activation of these receptors mediates a wide spectrum of biological activities including important changes in the central nervous system including satiety, control of circadian rhythm, thermoregulation, and in peripheral tissues including stimulation of gastrointestinal hormone release, activation of macrophages, and effects on development. Bn-related peptides also have potent growth effects causing proliferation of bothnormal cells and various tumor cell lines.
BRS-3 is receiving increased attention, because not only is it important in a number of gastrointestinal (GI) tract and central nervous system (CNS) processes, but also because it is one of the G-protein coupling receptor families most frequently ectopically or overexpressed by a different tumors, including prostate cancer, small cell lung cancer, breast cancer, CNS tumors, and carcinoids (intestinal, thymic, and bronchial).
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Bombesin Receptor Verwandte Produkte (55)
Verwandte Produkte (55)
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GRP (14-27) (human, porcine, canine)
0 ImagesArt. -Nr.: HY-P5072CAS. Nr.: 81608-29-9GRP (14-27) (human, porcine, canine) is a bombesin receptor ligand. The specific binding of GRP (14-27) is inhibited by GTP and GDP, whereas GMP was without effect. -
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AMBA
0 ImagesArt. -Nr.: HY-P11768CAS. Nr.: 721937-56-0AMBA is a gastrin-releasing peptide receptor (GRPR, BB2, BRS-2) ligand. AMBA binds to GRPR with high specificity and high affinity, and undergoes receptor-mediated endocytosis, which retains the conjugated radiometal in target cells. AMBA is applicable for the research of prostate cancer. -
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[D-Cys6,Asn7,D-Ala11,Cys14]-Bombesin (6-14)
0 ImagesArt. -Nr.: HY-P11408CAS. Nr.: 349657-39-2[D-Cys6,Asn7,D-Ala11,Cys14]-Bombesin (6-14), a synthetic peptide, is a non-selective bombesin receptor agonist. [D-Cys6,Asn7,D-Ala11,Cys14]-Bombesin (6-14) has preferred pEC50 values of 8.06 for the neurotrophin B bombesin receptor (BB1), 8.69 for the gastrin-releasing peptide bombesin receptor (BB2), and 6.71 for the orphan receptor (BB3). [D-Cys6,Asn7,D-Ala11,Cys14]-Bombesin (6-14) can be used to study diseases related to bombesin receptors, such as cancer and neurological disorders. -
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(D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P acetate
0 ImagesArt. -Nr.: HY-P3225CAS. Nr.: 143077-65-0(D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P (acetate) is an antagonist for Substance P (HY-P0201) and Bombesin (HY-P0195) that has effects on ocular inflammatory responses to antidromic trigeminal nerve stimulation. -
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GRPR antagonist-2
0 ImagesArt. -Nr.: HY-115975CAS. Nr.: 3052544-42-7GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity. -
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BIM 23042
0 ImagesArt. -Nr.: HY-103277CAS. Nr.: 111857-96-6BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin?B?(HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca2+ release. -
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PD 165929
0 ImagesArt. -Nr.: HY-125075CAS. Nr.: 185215-75-2PD 165929 is a high affinity and competitive non-peptide neuromedin-B (NMB) receptor selective antagonist (Ki: 6.3 nM; IC50: 150 nM for rat NMB receptor). -
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DSO-5a
0 ImagesArt. -Nr.: HY-154985CAS. Nr.: 2195411-63-1DSO-5a is a potent, selective, orally active BB3 agonist. DSO-5a is a representative DMAKO-00 derivative compound. DSO-5a upregulates ppar-γ activity through BB3 and activates ERK1/2 phosphorylation. DSO-5a can be used in diabetes-related research. -
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BIM187
0 ImagesArt. -Nr.: HY-103279CAS. Nr.: 137734-88-4BIM187 is a Bombesin Receptor agonist that induces satiety. BIM187 significantly reduces short-term food intake in rats, but does not alter the total 6 h food intake of rats. BIM187 can be used in studies related to feeding behavior and satiety regulation in rats. -
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PD176252 (Standard)
0 ImagesArt. -Nr.: HY-103286RCAS. Nr.: 204067-01-6PD176252 (Standard) is the analytical standard of PD176252 (HY-103286). This product is intended for research and analytical applications. PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells. -
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- PSMA/GRPR ligand 1
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Imidazol-1-yl-acetic acid (Standard)
0 ImagesImidazol-1-yl-acetic acid (Standard) is the analytical standard of Imidazol-1-yl-acetic acid (HY-W010448). This product is intended for research and analytical applications. Imidazol-1-yl-acetic acid is a BRS-3 agonist that mediates anorectic effects through activation of orphan G protein-coupled receptors (Orphan GPCR) in peripheral tissues; it also serves as a green, water-soluble, recyclable bifunctional organocatalyst for transformations such as the Biginelli multicomponent reaction and epoxide ring opening. Imidazol-1-yl-acetic acid can be used for research on obesity. -
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Nepitrin (Standard)
0 ImagesNepitrin (Standard) (Nepetin-7-glucoside (Standard)) is the analytical standard of Nepitrin (HY-N5010). This product is intended for research and analytical applications. Nepitrin (Nepetin-7-glucoside) is an orally active bradykinin and angiotensin antagonist isolated from Scrophularia striata. Nepitrin antagonizes the spasmogenic effects of Bradykinin and Angiotensin, thereby inhibiting inflammatory mediator pathways. Nepitrin is applicable to arthritis-related research. -
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Kuwanon G (Standard)
0 ImagesArt. -Nr.: HY-N4247RCAS. Nr.: 75629-19-5Kuwanon G (Standard) is the analytical standard of Kuwanon G (HY-N4247). This product is intended for research and analytical applications. Kuwanon G is a flavonoid compound and an antagonist of the bombesin receptor. Kuwanon G has multiple activities such as bactericidal, anti-tumor, anti-inflammatory, antioxidant, anti-atherosclerotic, and neuroprotective effects. Kuwanon G exhibits strong antibacterial activity against oral pathogens, especially cariogenic bacteria and periodontal pathogens. Kuwanon G can induce apoptosis and inhibit proliferation, migration, and invasion of tumor cells. Kuwanon G can be used in the research of diseases such as gastric cancer and atherosclerosis. -
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GRPR antagonist-3
0 ImagesArt. -Nr.: HY-180434CAS. Nr.: 2077238-49-2GRPR antagonist-3 (compound (S)-1m) is a potent GRPR antagonist with an IC50 of 121 nM. GRPR antagonist-3 is stable in rat plasma and towards microsomal oxidative metabolism in vitro. GRPR antagonist-3 can be radiolabeled with fluorine-18 for PET imaging. -
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