Endocrinology/Hormones

<p>PTH 13-34 is a biologically active fragment of parathyroid hormone (PTH) with hypertensive activities. PTH 13-34 is being trialled as a possible treatment for osteoporosis (to replace the existing recombinant human PTH 1-34 treatment peptide).PTH is an 84-amino-acid polypeptide hormone (PTH 1-84) which is secreted by the parathyroid glands along with its fragments (such as PTH 1-34 and PTH 7-84). PTH increases calcium and decrease phosphate levels in the blood and the abundance of PTH-derived peptides is regulated by blood calcium levels. PTH inhibits the bone growth-promoting activity of osteoblasts and induces osteoclasts to resorb bone and release calcium and phosphate ions into the blood. PTH binds to and activates the receptor parathyroid hormone receptor 1 (PTHR1). PTHR1 is a G-protein-coupled receptor (GPCR) which regulates mineral ion homeostasis, bone turnover and skeletal development.</p>

<p>Residues 1-12 of the gastrointestinal hormone motilin, secreted from endocrine cells in the small intestines, mainly from the jejunum and duodenum, in response to the fasting, drinking water or the mechanical stimulus of eating.</p>

<p>Calcitonin is a peptide hormone excreted by the thyroid parafollicular cells to regulate calcium and phosphorus levels. Calcitonin acts in opposition to parathyroid hormone (PTH) and vitamin D. Calcitonin functions by inhibiting osteoclast activity in the bones preventing calcium release- there is also inhibition of renal tubular cell reabsorption of calcium and phosphate, so they are excreted preventing a rise in levels.Calcitonin is used for as marker for detection and prognosis of nodular thyroid diseases. Medullary thyroid cancer is one example of the malignant parafollicular cells detectable with the assay, as they present with an increased calcitonin level even at an early stage.Since the discovery of calcitonin over 50 years ago the salmon sourced peptide has been used in numerous treatments including bone metastases, Paget disease, hypercalcaemia, and postmenopausal osteoporosis. The salmon calcitonin has been shown to be equivalent to human form but more active and can be synthetically generated.</p>

<p>Pro B-type natriuretic peptide (Pro-BNP) is secreted from cardiac myocytes and cleaved into BNP and the remaining part of the prohormone N-terminal proBNP (NT-proBNP). When the heart fibres become stretched more BNP and NT-proBNP are released to try and compensate for the increased pressure. During heart failure the walls of the atria become over stretched and thus increase the levels of NT-proBNP detectable. NT-proBNP has a longer half-life than BNP and therefore is detectable at higher levels in blood plasma than BNP. NT-pro-BNP is believed to be cleared by renal excretion, but this is not confirmed. As a diagnostic tool, NT-proBNP (47-76) has become very useful in helping diagnose heart failure and provide a prognosis. The measurement of NT-proBNP (47-76) has been incorporated into management and guidelines of clinical settings. As a research tool it still provides valuable data such as symptoms onset in relation to NT-proBNP levels and how inflammation effects the level of BNP as well as the BNP/ NT-proBNP ratio.</p>

<p>Vasopressin is a peptide antidiuretic hormone, originating from the hypothalamus, that regulates water balance in the body. It is also known as arginine vasopressin or antidiuretic hormone (ADH). The clinical efficacy of vasopressin has been evaluated using in vitro methods on mouse monoclonal antibody production cells, blood sampling, and microdialysis probes for monitoring blood pressure. This product is available in the salt form: Acetate.</p>

<p>Peptide derived from the gastrointestinal hormone Motilin, secreted from endocrine cells in the small intestines, mainly from the jejunum and duodenum, in response to the fasting, drinking water or the mechanical stimulus of eating.</p>

<p>Peptide derived from the Gastric inhibitory polypeptide (GIP), an inhibiting hormone of the secretin family of hormones. While GIP is a weak inhibitor of gastric acid secretion, its main role is to stimulate insulin secretion - in a glucose-dependent mechanism. Therefore, GIP is referred to as a glucose-dependent insulinotropic peptide.GIP is derived from a 153-amino acid pro-protein encoded by the GIP gene and circulates as a biologically active 42-amino acid peptide. It is synthesised by K cells, which are found in the mucosa of the duodenum and the jejunum of the gastrointestinal tract. GIP receptors are seven-transmembrane proteins found on β-cells in the pancreas. These β-cells are those that are able to simultaneously detect glucose and release insulin as a result to GIP binding.The clinical relevance of GIP is related to type 2 diabetes mellitus (T2DM)- studies have found that T2DM diabetics are unresponsive to GIP and have lower levels of GIP secretion after a meal when compared to non-diabetics. In research involving knockout mice, it was found that absence of the GIP receptors correlates with resistance to obesity.</p>

<p>Natural cleavage product of GLP-1 which, unlike GLP-1, does not affect either insulin secretion or glucose homeostasis.  GLP-1(9-36) has low affinity for, and acts as an antagonist to, the GLP-1 receptor.GLP-1 (9-36) does however display unique biological activities such as beneficial cardiovascular effects and reducing the production of reactive oxygen species (ROS). GLP-1 (9-36) also exerts important physiological effects on neuronal plasticity in the hippocampus, and inhibits chemokine-induced migration of human CD4-positive lymphocytes.GLP-1 (9-36) is formed from the breakdown of biologically active but highly unstable GLP-1 (7-36) amide by the ubiquitous serine protease, dipeptidyl peptidase-IV (DPP-IV).</p>

<p>ANP (7-23) is derived from the atrial natriuretic peptide (ANP) which is a cardiac hormone involved in maintaining cardio-renal homeostasis. This occurs through the activation of the guanylyl cyclase-coupled receptor, resulting in the increased concentration of cyclic guanylate monophosphate. Moreover its function in the processes of anti-proliferation and anti-angiogenesis allow it to take part in the cardiovascular remodelling process.ANP is a member of the natriuretic peptide family and it is encoded by the NPPA gene, located on chromosome 1. Once synthesized from the 151 amino acid pre-prohormone into its biologically active form, ANP is secreted by the atrial cardiomyocytes in the circulating forms: ANP (1-98) and ANP (99-126). This synthesis process involves the signal peptide being removed from the pre-prohormone resulting in proANP (1-126) which is converted into the circulating forms by the type II transmembrane serine protease Corin.</p>

<p>Gastric inhibitory polypeptide (GIP) is an inhibiting hormone of the secretin family of hormones. While GIP is a weak inhibitor of gastric acid secretion, its main role is to stimulate insulin secretion - in a glucose-dependent mechanism. Therefore, GIP is referred to as a glucose-dependent insulinotropic peptide. In GIP (Pro 3) the glutamic acid at position 3 has been substituted for a proline.GIP is derived from a 153-amino acid proprotein encoded by the GIP gene and circulates as a biologically active 42-amino acid peptide. It is synthesised by K cells, which are found in the mucosa of the duodenum and the jejunum of the gastrointestinal tract. GIP receptors are seven-transmembrane proteins found on β-cells in the pancreas. These β-cells are those that are able to simultaneously detect glucose and release insulin as a result to GIP binding.The clinical relevance of GIP is related to type 2 diabetes mellitus (T2DM)- studies have found that T2DM diabetics are unresponsive to GIP and have lower levels of GIP secretion after a meal when compared to non-diabetics. In research involving knockout mice, it was found that absence of the GIP receptors correlates with resistance to obesity.</p>

<p>This 32 amino acid peptide contains a 17 amino acid ring structure that is common to all natriuretic peptides. It is also called the brain natriuretic peptide (BNP) because it was first identified in porcine brain- however, the main source of this peptide is not the brain but the cardiac ventricle. This cardiac neurohormone is secreted from the ventricles in response to volume expansion and pressure overload. It has natriuretic and vasodilatory effects and suppresses the renin-angiotensin-aldosterone system.</p>

<p>ANP (1-23) is derived from the atrial natriuretic peptide (ANP) which is a cardiac hormone involved in maintaining cardio-renal homeostasis. This occurs through the activation of the guanylyl cyclase-coupled receptor, resulting in the increased concentration of cyclic guanylate monophosphate. Moreover its function in the processes of anti-proliferation and anti-angiogenesis allow it to take part in cardiovascular remodelling.ANP is a member of the natriuretic peptide family and it is encoded by the NPPA gene, located on chromosome 1. Once synthesized from the 151 amino acid pre-prohormone into its biologically active form, ANP is secreted by the atrial cardiomyocytes in the circulating forms: ANP (1-98) and ANP (99-126). This synthesis process involves the signal peptide being removed from the pre-prohormone resulting in pro-ANP (1-126) which is converted into the circulating forms by the type II transmembrane serine protease Corin.</p>

<p>Glucagon-like peptide (GLP) 1 is a post-translationally modified version of proglucagon. GLP-1 (1-37) is a naturally produced analog of GLP-1. Unlike truncated GLP-1, GLP-1 (1-37) does not alter food intake in rat models or pancreatic insulin secretion. GLP-1 (1-37) can induce insulin production in developing adult intestinal cells via upregulation of the ngn3 gene and its downstream targets. This can restore glucose homeostasis when implanted into diabetic mice. GLP-1 (1-37) may offer a  future treatment for diabetes mellitus. GLP-1 (1-37) can also inhibit chemokine-induced migration of human CD4-positive lymphocytes, an early step in atherogenesis. This raises the possibility that GLP-1 (1-37) is part of a novel mechanism to modulate vascular disease.</p>

<p>The cleavage of proglucagon forms glucagon. Increased levels of glucagon that can't be regulated are linked to diabetic hyperglycaemia and other pathologies. Typically, glucagon levels should be suppressed as glucose levels rise. However, the opposite has generally been found to be accurate, and the nature of this elevated immunoreactive glucagon has led to more research. Hyperglucagonaemia is a characteristic of several pathologies, but the detection of immunoreactive glucagon has yet to be fully verified due to the nature of available detection.Glucagon can be hydrolysed by dipeptidyl peptidase IV (DPIV) to products such as (18-29) and (3-29). Current methods for detecting glucagon rely on antibodies to the N terminus or  C-terminus to detect pancreatic glucagon. However, these antibodies may also detect truncated forms due to a pathology affecting the secretion, clearance or processing of proglucagon-derived peptides. Theoretically, these can be used in a sandwich process to detect only full-length glucagon. Therefore, the availability of the truncated glucagon (3-29) as a control to test the sensitivity of the available antibodies and the ELISAs is useful. Plasma levels from hyperglucagonaemic patients and healthy counterparts were used as a control to test the commercial glucagon assays and ELISAs. The truncated glucagon (3-29) provided valuable information about the sensitivity and specificity of the antibodies that have been used as an industry standard for glucagon measurement. This truncated glucagon is vital in ensuring our research moves forward with more controls and fewer assumptions.</p>

<p>PTH 1-34, is a biologically active peptide fragment of parathyroid hormone (PTH). PHT 1-34 has been shown to enhance bone fracture healing by promoting osteogenesis. PTH 1-34 also has chondrogenic properties.PTH is an 84-amino-acid polypeptide hormone (PTH 1-84) which is secreted by the parathyroid glands along with its fragments (such as PTH 1-34 and PTH 7-84). PTH increases calcium and decrease phosphate levels in the blood and the abundance of PTH-derived peptides is regulated by blood calcium levels. PTH inhibits the bone growth-promoting activity of osteoblasts and induces osteoclasts to resorb bone and release calcium and phosphate ions into the blood. PTH binds to and activates the receptor parathyroid hormone receptor 1 (PTHR1). PTHR1 is a G-protein-coupled receptor (GPCR) which regulates mineral ion homeostasis, bone turnover and skeletal development.</p>

<p>Bradykinins and their associated kinins are inflammatory mediators produced during inflammation. The two main kinins in mammals are the nonapeptide bradykinin, BK (1-9) and the decapeptide kallidin (KD), [Lys0]-BK(1-10). Their biological actions are mediated by two distinct receptors, termed B1 and B2.-BK is involved in several pathophysiological processes, such as inflammation, pain, cell proliferation, and tumours. It plays a crucial role in corneal epithelial cells, corneal stromal cells, and fibroblasts.Inflammation has been reported as one significant hallmark of breast cancer in relation to tumour development, metastasis, and invasion. The bradykinin receptor 1 (B1R) associated with kallidin is highly expressed on inflammatory breast tumour cells thus providing a promising targeting site for tumour recognition and sufficient receptor mediated endocytosis.</p>

<p>ANP (13-26) is derived from the atrial natriuretic peptide (ANP) which is a cardiac hormone involved in maintaining cardio-renal homeostasis. This occurs through the activation of the guanylyl cyclase-coupled receptor, resulting in the increased concentration of cyclic guanylate monophosphate. Moreover its function in the processes of anti-proliferation and anti-angiogenesis allow it to take part in the cardiovascular remodelling process.ANP is a member of the natriuretic peptide family and it is encoded by the NPPA gene, located on chromosome 1. Once synthesized from the 151 amino acid pre-prohormone into its biologically active form, ANP is secreted by the atrial cardiomyocytes in the circulating forms: ANP (1-98) and ANP (99-126). This synthesis process involves the signal peptide being removed from the pre-prohormone resulting in proANP (1-126) which is converted into the circulating forms by the type II transmembrane serine protease Corin.</p>

<p>N-terminal tryptic peptide of parathyroid hormone (PTH), used for quantification and optimisation in LC-MS/MS assays.PTH is an 84-amino-acid polypeptide hormone (PTH 1-84) which is secreted by the parathyroid glands along with its fragments (such as PTH 1-34 and PTH 7-84). PTH increases calcium and decrease phosphate levels in the blood and the abundance of PTH-derived peptides is regulated by blood calcium levels. PTH inhibits the bone growth-promoting activity of osteoblasts and induces osteoclasts to resorb bone and release calcium and phosphate ions into the blood. PTH binds to and activates the receptor parathyroid hormone receptor 1 (PTHR1). PTHR1 is a G-protein-coupled receptor (GPCR) which regulates mineral ion homeostasis, bone turnover and skeletal development</p>

<p>ANP (9-22) is derived from the atrial natriuretic peptide (ANP) which is a cardiac hormone involved in maintaining cardio-renal homeostasis. This occurs through the activation of the guanylyl cyclase-coupled receptor, resulting in the increased concentration of cyclic guanylate monophosphate. Moreover its function in the processes of anti-proliferation and anti-angiogenesis allow it to take part in the cardiovascular remodelling process.ANP is a member of the natriuretic peptide family and it is encoded by the NPPA gene, located on chromosome 1. Once synthesized from the 151 amino acid pre-prohormone into its biologically active form, ANP is secreted by the atrial cardiomyocytes in the circulating forms: ANP (1-98) and ANP (99-126). This synthesis process involves the signal peptide being removed from the pre-prohormone resulting in proANP (1-126) which is converted into the circulating forms by the type II transmembrane serine protease Corin.</p>

<p>This is an incretin hormone that causes glucose dependent release of insulin by pancreatic beta cells. It is the cleavage product of GLP-1 (1-36) amide peptide.  This peptide, human GLP-1 (7–36), shares the same sequence with preproglucagon (78-107), amide, human.</p>

<p>Fulvestrant-d3 is a isotope labeled compound of Fulvestrant.an estrogen receptor (ER) antagonist and GPR30 agonist thatinduces apoptosis and autophagy.</p>

Estrone-d4 3-Sulfate Sodium Salt is a deuterated compound of Estrone 3-Sulfate Sodium Salt. Estrone 3-Sulfate Sodium Salt has a CAS number of 438-67-5.

<p>Estrone-d2 is a deuterated compound of Estrone. Estrone has a CAS number of 53-16-7. Estrone is an aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from ANDROSTENEDIONE directly, or from TESTOSTERONE via ESTRADIOL. In humans, it is produced primarily by the cyclic ovaries, PLACENTA, and the ADIPOSE TISSUE of men and postmenopausal women.</p>

<p>Lisinopril, an ACE inhibitor, treats hypertension, heart failure, heart attacks, and prevents diabetes-related eye and kidney issues.</p>

<p>AR antagonist 6 (compound 6i), a diphenyl ether androgen receptor (AR) antagonist, binds to the AR with an affinity of 120 nM. It demonstrates low toxicity and effective in vitro activity in the golden Syrian hamster ear model. [19] [1]</p>

<p>Fenclofenac: a non-steroidal anti-inflammatory that blocks T4 and T3 binding to TBG.</p>

<p>GDC-2992 is a selective androgen receptor (AR) degradator that degrades AR and inhibits proliferation in VCaP cells,CRPC.</p>

<p>T3-ATA S-isomer, the S-isomer of T3-ATA, represents the active form of the thyroid hormone.</p>

<p>GRT2932Q is a nonpeptidic agonist of the opioid receptor-like 1 (ORL1) [1].</p>

<p>Estromustine, an active metabolite of estramustine phosphate, is used to treat prostate cancer.</p>

<p>ASN04885796 is a neuroprotective, specific GPR17 agonist with an EC50=2.27 nM for GPR17-mediated GTPγS binding and study neurodegenerative diseases</p>

<p>L-6424 is an intermediate of Amiodarone and a non-selective ion channel blocker. It has an antiarrhythmic.</p>

<p>CGP-53153 is a steroidal inhibitor of 5 alpha-reductase (IC50s: 36 and 262 nM in rat and human prostatic tissue).</p>

A 274 is a highly aromatic, monosubstituted phenol antioxidant generated during differentiation of neuroblastoma cells.

<p>Originally identified in Gila monster lizard (Heloderma suspectum), exendin-4 is an incretin mimetic, an analog of glucagon-like-peptide-1 (GLP-1), it stimulates insulin secretion and modulates gastric emptying to slow the entry of ingested sugars into the bloodstream. Exendin-4 is resistant to cleavage by plasma DPP-IV unlike GLP-1. This gives it a longer half-life and duration of action than GLP-1, as well as greater potency in vivo. Exendin-4 increases insulin sensitivity and improves glucose tolerance and is currently used for the treatment of Type 2 diabetes mellitus in its synthetic form Exenatide. Exendin-4 also promotes the production and proliferation of beta-cells leading to regeneration of the pancreas. It is a ligand to the exendin receptor and increases pancreatic acinni cAMP levels. However, the GLP-1 analog was found to have a toxic effect by inducing hypotension due to relaxation of the cardiac smooth muscle.</p>

Irbesartan-d4 (Irbesartan D4), a deuterated compound of Irbesartan, is an angiotensin receptor blocker and is used in the study of cardiovascular disease.

<p>3,3',5-Triiodothyronine-(tyrosine ring-13C6) is the 13C labeled compound of 3,3',5-Triiodothyronine. 3,3',5-Triiodothyronine has a CAS number of 5817-39-0.</p>

<p>Losartan D4: deuterium-enriched Losartan, an angiotensin II blocker, with a 20 nM IC50.</p>

<p>JNJ-37654032: orally active, nonsteroidal SARM. Mixed AR agonist/antagonist. Selective for muscle, grows levator ani, max at 3mg/kg, ED(50) 0.8mg/kg.</p>

Cilazapril Monohydrate (Justor) is an angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and congestive heart failure.

Timobesone is a topical corticosteroid.

<p>Diisopropyl phthalate is widely used as an additive in plastics and consumer products in the chemical industries.</p>

<p>4'-Raloxifene-β-D-glucopyranoside is a metabolite of Raloxifene.</p>

<p>VTP-27999 is an alkyl amine Renin inhibitor. VTP-27999 has been used in trials studying the basic science of Renal Function.</p>

<p>4-Hydroxytoremifene is a selective estrogen receptor modulator toremifene active metabolite.</p>

<p>Procymidone is a broad-spectrum fungicide that inhibits fungal glycerol triester synthesis, thereby disrupting hyphal growth. androgen receptor (AR) antagonist</p>

<p>Endoxifen E-isomer hydrochloride (E-Endoxifen hydrochloride) , a tamoxifen metabolite, is effective specific Estrogen Response Modifier (SERM).</p>

<p>Originally identified in Heloderma horridum horridum (Mexican beaded lizard), exendin-3 is in the glucagon family. Exendin 3 stimulates vasoactive intestinal peptide (VIP) receptors in high concentrations. This leads to increased cAMP levels and amylase secretion in the pancreas. However, low exendin-3 exposure only increases cAMP levels. In applications, exendin-3 was found to induce hypotension by relaxation of cardiac, smooth muscle. Using a tag, exendin-3 is being investigated as a stable agonist for GLP1R to detect insulinomas, a pancreatic B cell-derived cancer with high GLP1R expression. Exendin 3 has also been used on mouse models to assess its effect on glucose-stimulated insulin secretion in glucagon receptor knockout (Gcgr-/-) backgrounds. Understanding the interplay between exendin 3 and metabolism could provide new insights into the obesity crisis.</p>

Palosuran (ACT-058362) (ACT-058362) is a new potent and specific antagonist of the human UT receptor.

<p>Lipidated Oxytocin analog with long-lasting activities. Product has the following disulfide bonds: Cys1-Cys6 and is available as a 0.5mg vial.</p>