insulin (human)

Insulin (human) is a peptide hormone that promotes glycogen synthesis and regulates glucose levels in the blood. Insulin (human) has hypoglycemic activity and is used clinically to treat hyperglycemia in diabetic patients.

GIP (3-42), human (Gastric Inhibitory Polypeptide (3-42) (human)) is a peptide that acts as a glucose-dependent proinsulinotropic polypeptide (GIP) receptor antagonist and regulates insulin secretion and the metabolic effects of GIP in vivo, which can be used to study type 2 diabetes.

S961 is a high-affinity, selective insulin receptor (IR) antagonist with IC50 values of 0.048 nM for HIR-A, 0.027 nM for HIR-B, and 630 nM for human insulin-like growth factor I receptor (HIGF-IR) in scintillation proximity assays.

This peptide is a fragment of the alpha-chain of insulin amino acids 1 to 13. The insulin a-chain epitope recognized by human T cells is posttranslationally modified.

GIP (3-42), human acetate is an antagonist of a glucose-dependent insulinotropic polypeptide (GIP) receptor and regulates insulin secretion and GIP metabolism in vivo.

Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004). Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3 References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004).

Selective VPAC2 receptor agonist (EC50 values are 0.4, 100 and >1000 nM for VPAC2, VPAC1 and PAC1, respectively in a cAMP accumulation assay; IC50 values are 60, 8700 and >10000 nM for VPAC2, VPAC1 and PAC1, respectively in a competition binding assay). S

Neuromedin U (NMU) is a neuropeptide first demonstrated to drive smooth muscle contraction.1Translated as a 174 amino acid propeptide, NMU is cleaved to different lengths in different animals. It has diverse receptor-mediated rolesin vivo, as it regulates feeding, vasoconstriction, nociception, and bone remodeling and contributes to obesity, cancer and septic shock.2,2NMU-25 is the active form of NMU in humans. It binds with high affinity to receptors on human left ventricle and coronary artery (KDs = 0.26 and 0.11 nM, respectively), eliciting endothelium-independent vasoconstriction.3NMU-25 also suppresses glucose-stimulated insulin secretion in human islets, and this effect is lost in NMU R165W mutants, resulting in early-onset obesity.4 1.Mitchell, J.D., Maguire, J.J., and Davenport, A.P.Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin SBritish Journal of Pharmacology15887-103(2009) 2.Greenwood, H.C., Bloom, S.R., and Murphy, K.G.Peptides and their potential role in the treatment of diabetes and obesityRev.Diabet.Stud.8(3)355-368(2011) 3.Mitchell, J.D., Maguire, J.J., Kuc, R.E., et al.Expression and vasoconstrictor function of anorexigenic peptides neuromedin U-25 and S in the human cardiovascular systemCardiovascular Research81353-361(2009) 4.Alfa, R.W., Park, S., Skelly, K.R., et al.Suppression of insulin production and secretion by a decretin hormoneCell Metabolism21(2)323-333(2015)

Acetyl Gastric Inhibitory Peptide (human) TFA, a fatty acid-derivatized analog of the glucose-dependent insulinotropic polypeptide, exhibits enhanced antihyperglycemic and insulinotropic properties. It is utilized in the research of diabetes, insulin resistance, and obesity [1] [2] [3].

(Ser8)-GLP-1 (7-36) amide, human, is a glucagon-like peptide-1 amide derived from glucagonogen, a cleavage product of the GLP-1 (1-36) amide peptide. This entero-insulinotropic hormone promotes glucose-dependent insulin secretion from pancreatic β-cells and affects gastrointestinal motility and secretion [1].

GIP (1-30) amide, human acetate is a fragment of glucose-dependent insulinotropic polypeptide (GIP), an incretin hormone that plays a crucial role in stimulating insulin secretion and mitigating postprandial glycemic excursions. This compound has been shown to enhance insulin secretion in a dose-dependent manner across concentrations of 10^-9 to 10^-6 M [1].

S961 acetate is a selective and high-affinity antagonist of the insulin receptor (IR), demonstrating IC50 values of 0.048 nM for HIR-A, 0.027 nM for HIR-B, and 630 nM for the human insulin-like growth factor I receptor (HIGF-IR) in SPA assays [1].

Adropin (34-76) (human, mouse, rat) is a peptide that attenuates liver fibrosis and insulin resistance independent of obesity or food intake.

Amylin (8-37), human, derived from human Amylin, possesses direct vasodilator effects in isolated mesenteric resistance arteries of rats. Human Amylin is a small pancreatic β-cell hormone that forms aggregates in the absence of insulin and is a key pathological feature of type II diabetes mellitus.

Glucagon-like peptide 1 (1-37), human, is a highly potent agonist of the GLP-1 receptor and a pancreatic hormone synthesized by post-translational processing of proglucagon. Unlike truncated forms of GLP-1, it neither affects food intake in rats nor enhances pancreatic insulin secretion.

Osteocalcin (1-49) is a non-collagenous peptide that is secreted by osteoblasts and odontoblasts and comprises 1-2% of the total protein in bone. Secretion of osteocalcin (1-49) is stimulated by 1,25-dihydroxy vitamin D and plasma levels increase in diseases that induce dysregulated bone turnover such as osteoporosis, Paget's disease, and primary hyperparathyroidism. Osteocalcin (1-49) is positively correlated with insulin sensitivity and negatively correlated with high blood glucose levels in women. In vitro, osteocalcin induces chemotaxis of MDA-MB-231 breast cancer cells, human peripheral blood monocytes, and rat osteosarcoma cells with osteoblast-like characteristics. It is also expressed by vascular smooth muscle cells (VSMCs) displaying an osteoblast-like phenotype and has been positively associated with calcification of aortic tissue and heart valves in humans.

Galanin (1-30), human, is a 30-amino acid neuropeptide that acts as an agonist of GalR1 and GalR2 receptors with Kis of 1 nM for both. This endogenous peptide exhibits multiple endocrine, metabolic, and behavioral effects, influencing intestinal smooth muscle, insulin and somatostatin release, and synaptic neurotransmission.

Transdermal Peptide TD-1 HCl is a novel peptide for enhanced transdermal drug delivery that facilitates the penetration of the skin barrier by several drugs and large hydrophilic proteins, such as insulin and human growth hormoneb.

Amylin (1-37), human acetate (hIAPP (1-37), acetate), a peptide hormone containing 37 amino acids secreted by the pancreas in conjunction with insulin, inhibits glucagon secretion and produces satiety during glucose homeostasis, and is a major component of amyloid deposits in the pancreas of patients with type 2 diabetes.

MOTS-c(Human) Acetate is a mitochondrial-derived peptide. MOTS-c(human) acetate induces the accumulation of AMP analog AICAR, increases activation of AMPK and expression of its downstream GLUT4. MOTS-c(human) acetate induces glucose uptake and improves insulin sensitivity. MOTS-c(human) acetate has implications in the regulation of obesity, diabetes, exercise, and longevity.

PHM-27 (human) acetate is the endogenous peptide product of prepro-VIP (human), an agonist of the calcitonin receptor (EC 50 = 11 nM). Transgenic mice overexpressing PHM-27 (human) acetate in pancreatic β-islets exhibited enhanced glucose-induced insulin secretion.

S961 TFA is A high affinity insulin receptor (IR) antagonist with IC50 for hir-a, hir-b and human insulin-like growth factor I receptor (higf-ir) at 0.048, 0.027 and 630 nM, respectively.

Somatostatin, also known as growth hormone-inhibiting hormone, is a naturally-occurring peptide hormone of 14 or 28 amino acid residues that regulates the endocrine system. It is secreted by the D cells of the islets to inhibit the release of insulin and

Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.