Biological ActivityPotent bombesin receptor subtype 3 (BRS-3; BB3) agonist (IC50 = 2.52 nM). Also GRPR (BB1) and NMBR (BB2) agonist (IC50 values are 0.26 and 1.55 nM respectively). Enhances glucose transport in obese and diabetic primary myocytes. Also stimulates NCI-H1299 lung cancer cell proliferation in vitro.
(Modifications: Tyr-1= D-Tyr, Ala-6 = β-Ala, X = Nle, Nle-9 = C-terminal amide)
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth.
Moody et al.
Discovery of a high affinity radioligand for the human orphan receptor, bombesin receptor subtype 3, which demonstrates that it has a unique pharmacology compared with other mammalian bombesin receptors.
Mantey et al.
J Biol Chem., 1997;272:26062
Effect of bombesin receptor subtype-3 and its synthetic agonist on signaling, glucose transport and metabolism in myocytes from patients with obesity and type 2 diabetes
González et al.
Comparative pharmacology of bombesin receptor subtype-3, nonpeptide agonist MK-5046, a universal peptide agonist, and peptide antagonist Bantag-1 for human bombesin receptors.
Moreno et al.
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