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You are here:Home-Inhibitors & Agonists-GPCR-Bombesin Receptor

Request The Product List ofBombesin Receptor Bombesin Receptor

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.

Cat. No. Product Name CAS No. Information
H8682

RC-3095 trifluoroacetate

 		1217463-61-0

RC-3095 trifluoroacetate is a bombesin/gastrin releasing peptide receptor (GRPR) antagonist; RC-3095 exerts protective effects by reducing gastric oxidative injury in the arthritic mice.
H8379

(S)-BRS-3 agonist Compound A

 		2489622-02-6

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).
H3040

RC-3095

 		138147-78-1

RC-3095 is a bombesin/gastrin releasing peptide receptor (GRPR) antagonist; RC-3095 exerts protective effects by reducing gastric oxidative injury in the arthritic mice.
H3039

BRS-3 agonist Compound A racemate

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).
H3038

BRS-3 agonist Compound A

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
H3037

Bantag-1 trifluoroacetate

 		1972659-15-6

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.
H3036

(S)-BRS-3 agonist Compound A

 		2489622-02-6

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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