Bombesin a peptide of 14 amino acids, is an amphibian homolog to the mammalian gastrin-releasing peptide (GRP), that has been extensively studied as a targeting ligand for diagnosis and therapy of GRP positive tumors, such as breast, pancreas, lungs and prostate cancers. Bombesin binds to and activates G-protein coupled receptors, known as gastrin releasing peptide receptor (GRPR).
Bombesin, a tetradecapeptide isolated from the skin of the frog Bombina bombina, have shown broad spectrum of biological activities. The BBS activates three G protein-coupled receptors: bombesin receptor 1 (BB1), bombesin receptor 2 (BB2), and bombesin receptor 3 (BB3). BBS-like peptides-Neuromedin B (NB) and gastrin releasing peptide (GRP) are natural ligand of the BB1 and BB2 receptors, respectively.
In mammals, BBS receptors and BBS-like peptides are distributed in the Central Nervous System (CNS) including regions involved in the cardiorespiratory control.
The mammalian bombesin G-protein-coupled receptor subfamily comprises three structurally related members, the receptors for neuromedin B (NMBR or BB1), gastrin-releasing peptide (GRPR or BB2), and bombesin receptor subtype-3 (BRS-3 or BB3).
Bombesin receptor subtype-3 (BRS-3) is an orphan G protein-coupled receptor implicated in the regulation of energy homeostasis.
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RC-3095 (RC 3095;RC3095) is a potent, peptide bombesin/gastrin releasing peptide (GRPR,BRS-1) antagonist.
Bantag-1 trifluoroacetate is a potent, highly selective, peptide bombesin receptor subtype-3 (BRS-3) antagonist with IC50 of 2-8 nM for human and rodent BRS-3, displays 1000-fold selectivity over hNMBR and hGRPR, increases food intake and produces an obesity phenotype in mice.
BRS-3 agonist Compound A
BRS-3 agonist Compound A is a potent, selective, orally active bombesin receptor subtype-3 (BRS-3) agonist with EC50 of 250/100 nM for human/rat BRS-3, resp+H1437+M1438
BRS-3 agonist Compound A racemate
BRS-3 agonist Compound A racemate is a potent, selective, orally active bombesin receptor subtype-3 (BRS-3) agonist with EC50 of 270/130 nM for human/rat BRS-3, respectively; displays no activity against GRPR (BRS-1) and NMBR (BRS-2) (EC50>10 uM)
(S)-BRS-3 agonist Compound A
The distomer of BRS-3 agonist Compound A, shows no activity for bombesin receptor subtype-3 (BRS-3) with EC50>10 uM.
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