Bombesin Receptor Agonist

MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC₅₀ and an EC₅₀ value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity.

BA 1 TFA is a potent agonist for the bombesin (BB) family of receptors. BA1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC₅₀s of 6, 0.4, 2.5 nM.

Litorin, an amphibian bombesin peptide derivative, is an bombesin receptor agonist. Litorin stimulates the contraction of smooth muscle, stimulates gastrin, gastric acid, and pancreatic secretion, and suppresses the nutriment in vivo.

[Tyr4]-Bombesin is a Bombesin analogue, is a ligand of gastrin-releasing peptide receptor (GRPR).

MK-7725 is a selective, orally active, and blood-brain barrier-permeable agonist of the subtype 3 of the frog skin peptide receptor (BRS-3). MK-7725 has a high affinity for the human BRS-3 (hBRS-3), with an IC₅₀ of 3 nM, and its functional activity in the mouse-derived BRS-3 (mBRS-3) model with an EC₅₀ of 22 nM (105% agonistic). MK-7725 significantly reduces the body weight of obese rats and obese dogs. MK-7725 can be used for the treatment of obesity.

BRS-3 receptor agonist-2 (compound 2) is a potent BRS-3 receptor agonist, with an EC₅₀ of 2.5 nM for mouse BRS-3 receptor.

BA 1 is a potent agonist for the bombesin (BB) family of receptors. BA 1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC₅₀s of 6, 0.4, 2.5 nM.

GRP (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.

[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.

DSO-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.