(Des-octanoyl)-Ghrelin (human) (trifluoroacetate salt)

Ghrelin is an endogenous gastrointestinal hormone and neuropeptide that binds to the growth hormone (GH) secretagogue receptor (GHS-R).1,2 Ghrelin requires an n-octanoyl modification at serine 3 for binding to the growth hormone (GH) secretagogue receptor (GHS-R).3 (Des-octanoyl)-ghrelin (human) is a form of ghrelin that is lacking the octanoyl group at serine 3. It is located in the mouse stomach and is expressed at a lower level than octanoyl ghrelin.4 (Des-octanoyl)-ghrelin activates GHS-R by only 41% when used at 10 µM (IC50 = >10,000 nM; EC50 = >10,000 nM for increasing calcium accumulation).5 It induces bone marrow adipogenesis in rat models of growth hormone deficiency.6 (Des-octanoyl)-ghrelin also inhibits cell proliferation in estrogen-dependent MCF-7 breast cancer cells (EC50 = 0.81 µM) but induces proliferation of a somatotroph pituitary tumor cell line, an effect that can be blocked by MAPK, PKC, and tyrosine kinase inhibitors.7,8WARNING This product is not for human or veterinary use.

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[2] SUZANNE L. DICKSON . The role of the central ghrelin system in reward from food and chemical drugs[J]. Molecular and Cellular Endocrinology, 2011, 340 1: Pages 80-87. DOI: 10.1016/j.mce.2011.02.017
[3] RESH M D. Fatty acylation of proteins: The long and the short of it[J]. Progress in lipid research, 2016, 63: Pages 120-131. DOI: 10.1016/j.plipres.2016.05.002
[4] SARA JANSSEN. Bitter taste receptors and α-gustducin regulate the secretion of ghrelin with functional effects on food intake and gastric emptying.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2011: 2094-2099. DOI: 10.1073/pnas.1011508108
[5] MARIA A. BEDNAREK. Structure−Function Studies on the New Growth Hormone-Releasing Peptide, Ghrelin: Minimal Sequence of Ghrelin Necessary for Activation of Growth Hormone Secretagogue Receptor 1a⊥[J]. Journal of Medicinal Chemistry, 2000, 43 23: 4370-4376. DOI: 10.1021/jm0001727
[6] NICHOLA M THOMPSON. Ghrelin and des-octanoyl ghrelin promote adipogenesis directly in vivo by a mechanism independent of the type 1a growth hormone secretagogue receptor.[J]. Endocrinology, 2004, 145 1: 234-242. DOI: 10.1210/en.2003-0899
[7] P. CASSONI. Identification, characterization, and biological activity of specific receptors for natural (ghrelin) and synthetic growth hormone secretagogues and analogs in human breast carcinomas and cell lines.[J]. Journal of Clinical Endocrinology & Metabolism, 2001, 163 1: 1738-1745. DOI: 10.1210/jcem.86.4.7402
[8] ALEXANDRA M NANZER. Ghrelin exerts a proliferative effect on a rat pituitary somatotroph cell line via the mitogen-activated protein kinase pathway.[J]. European Journal of Endocrinology, 2004, 151 2: 233-240. DOI: 10.1530/eje.0.1510233