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Alarelin acetate is a synthetic LH-RH agonist, and stimulates the release of FSH and LH from the pituitary gland. It is known for its induction of ovulation and used to treat endmometriosis.
Glucagon-like peptide-1 (GLP-1) is an incretin derived from the transcription product of the proglucagon gene. The major source of GLP-1 in the body is the intestinal L cell that secretes GLP-1 as a gut hormone. Its physiological functions include promoting insulin sensitivity, decreasing food intake by increasing satiety in brain and increasing insulin secretion from the pancreas in a glucose-dependent manner.
Abarelix is a synthetic decapeptide antagonist to gonadotropin releasing hormone (GnRH). It directly and competitively binds and blocks the gonadotropin releasing hormone receptors in the anterior pituitary, which inhibits the secretion and release of the luteinizing hormone (LH) and follicle stimulating hormone (FSH). For men, the inhibition of LH secretion prevents the release of testosterone. Therefore, it can relieve symptoms associated with prostate hypertrophy or prostate cancer.
Glucagon (Porcine glucagon) is a peptide hormone, produced by pancreatic α-cells. Glucagon stimulates gluconeogenesis. Glucagon decreases the activity of HNF-4. Glucagon increases HNF4α phosphorylation.
Bivalirudin, a peptide anticoagulant, is a direct thrombin inhibitor for anticoagulation in the setting of invasive cardiology, particularly percutaneous coronary intervention.
Aviptadil, also known as vasoactive intestinal polypeptide (VIP), is a 28 amino acid neuropeptide that belongs to the glucagon-growth hormone-releasing factor secretion superfamily. Aviptadil acts as a potent systemic vasodilator and bronchodilator. It inhibits the proliferation of vascular and bronchial smooth muscle cells and decreases platelet aggregation. These biological effects are mediated by specific VIP receptors.
Angiotensin II is an octapeptide that produced from angiotensin I after the removal of two amino acids at the C-terminal by angiotensin-converting enzyme (ACE). Angiotensin II is mediated by AT1 and AT2 receptors, which are seven transmembrane glycoproteins with 30% sequence similarity.
Terlipressin is a synthetic triglycyllysine derivative of vasopressin with vasoconstrictive, antihemorrhagic, and antidiuretic properties. Upon intravenous administration, terlipressin, an inactive prodrug, is biotransformed to its active moiety, lysine vasopressin (LVP), a nonselective vasopressin analogue with affinity for vasopressin receptors V1 (V1a), V2 and V3 (V1b). As a V1 agonist, terlipressin increases systemic vascular resistance, particularly in the splanchnic area, resulting in a decrease of portal pressure. V1 binding also promotes platelet aggregation and glycogenolysis, while V3 binding induces adrenocorticotropic hormone (ACTH) secretion. Compared to vasopressin, terlipressin has a minimal effect on V2 receptors, which are responsible for promotion of water reabsorption in the collecting ducts of the kidney via stimulation of cyclic AMP production.
Goserelin acetate stimulates the production of the sex hormones testosterone and estrogen in a non-pulsatile (non-physiological) manner. This causes the disruption of the endogenous hormonal feedback systems, resulting in the down-regulation of testosterone and estrogen production.
Thymopentin, also known as TP-5, is a synthetic derivative of thymopoietin, a thymic hormone, and has immunoregulatory properties. Thymopentin interacts with T cells, reduces endocrine and behavioral responses to experimental stress. It is also found to increase the number of cells undergoing apoptosis in irradiated cells and selectively bind to apoptotic cells.