GRF (1-44) (HUMAN) CAS 83930-13-6

Introduction:Basic information about GRF (1-44) (HUMAN) CAS 83930-13-6, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

GRF (1-44) (HUMAN) Basic informationStructure Gene, mRNA, and precursor Synthesis and release Synthesis and release Receptors Agonists and Antagonists Biological functions Clinical implications Description Background

Product Name:GRF (1-44) (HUMAN)
Synonyms:SERMORELIN (HUMAN);SOMATOCRININ (HUMAN);SOMATOLIBERIN (HUMAN);SOMATORELIN;YADAIFTNSYRKVLGQLSARKLLQDIMSRQQGESNQERGARARL-NH2;TYR-ALA-ASP-ALA-ILE-PHE-THR-ASN-SER-TYR-ARG-LYS-VAL-LEU-GLY-GLN-LEU-SER-ALA-ARG-LYS-LEU-LEU-GLN-ASP-ILE-MET-SER-ARG-GLN-GLN-GLY-GLU-SER-ASN-GLN-GLU-ARG-GLY-ALA-ARG-ALA-ARG-LEU-NH2;GRF (huMan)SoMatoliberin (huMan), SoMatocrinin (huMan), SoMatorelin (huMan), Growth HorMone-Releasing Factor (huMan), Growth HorMone-Releasing HorMone (huMan), GHRH (huMan), SoMatorelin;SoMatoliberin (huMan), SoMatocrinin (huMan), SoMatorelin (huMan), Growth HorMone-Releasing Factor (huMan), Growth HorMone-Releasing HorMone (huMan), GHRH (huMan), SoMatorelin
CAS:83930-13-6
MF:C215H358N72O66S
MW:5039.65082
EINECS:
Product Categories:Peptide;VIP and PACAP receptor;peptides pharm
Mol File:83930-13-6.mol

GRF (1-44) (HUMAN) Chemical Properties

storage temp. −20°C
form powder
color White to off-white
Water Solubility Water : 25 mg/mL (4.96 mM)
SequenceTyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu-NH2
InChIKeyJAHCMOSSKRAPEL-IBFVROBCSA-N

Safety Information

WGK Germany 3

GRF (1-44) (HUMAN) Usage And Synthesis

StructureGHRH(1–29) is the bioactive core of human GHRH. The N-terminal tyrosine residue withselected aromatic rings is important for the high bioactivity in human and nonrodent mammalian GHRH. The amino acid sequence of GHRH shows higher identities between the human, porcine, bovine, and caprine species, but the rat and mouse are exceptions. Thesequence of the C-terminus is highly variable among species while the N-terminus is more conserved. The N-terminal region (1–27) of GHRH is well conserved in nonmammalian vertebrates. Zebrafish GHRH(1–27) shows 74.1%, 81.5%, and 81.5% similarity to theXenopus tropicalis, chicken, and human counterparts,respectively. Mr 12,447 (GHRH(1-44), Mr 5,039), pI 10.3 (GHRH(1-44), pI 11.5). Soluble in acidic aqueous solution (e.g., 1%acetic acid). Lyophilized GHRH is stable at room temperature for 2months, and recommended storage is below-18°C with desiccation.
Gene, mRNA, and precursorThe human GHRH gene, GHRH, location 20q11.2, consists of five exons. GHRH mRNA has 459 bases thatencode a signal peptide of 24 aa residues, a mature protein of 44 aa residues, and a C-peptide of 31 aa residueswith unknown function. In nonmammalianvertebrates, the GHRH-like peptide and PACAP werefirst believed to be encoded by the same gene, but lateractual GHRH and PACAP were found to be encodedby two distinct genes.
Synthesis and releaseThe human GHRH gene, GHRH, location 20q11.2, consists of five exons. GHRH mRNA has 459 bases thatencode a signal peptide of 24 aa residues, a mature protein of 44 aa residues, and a C-peptide of 31 aa residueswith unknown function. In nonmammalianvertebrates, the GHRH-like peptide and PACAP werefirst believed to be encoded by the same gene, but lateractual GHRH and PACAP were found to be encodedby two distinct genes.
Synthesis and releaseThe synthesis and release of GHRH are regulated bysex hormones, aging, the negative feedback effect ofGH, and diverse pathological conditions. Gsh-1 has beenconsidered a transcriptional factor of Ghrh expression inthe rat hypothalamus. GHRH synthesis is inhibited bysomatostatin (SS). The expression levels of the SS receptor, sst2A, in GHRH neurons are higher in female micethan male mice. The production of hypothalamic GHRHis decreased by aging. It is also negatively regulated bythe feedback of GH, whereas ghrelin stimulates GHRHrelease.
ReceptorsGHRH-R belongs to the GPCR B II subclass, highlyselective for GHRH. The GHRH-R of most mammalsconsists of 423 aa residues. The N-terminal extracellulardomain contains a site for N-glycosylation as well assix cysteine residues and an aspartate residue that areconserved in this receptor family. The third intracellularloop and the C-terminal intracellular domain contain several potential phosphorylation sites, which may regulatesignaling and receptor internalization. It is mainlyexpressed in the pituitary.
Agonists and AntagonistsTesamorelin, sermorelin (GHRH(1–29)-NH2), andCJC-1295 are agonists. Antagonists comprise the antibodies or peptides toGHRH-R: JV-1-10, JV-1-36, JV-1-37, JV-1-38, JV-1-39,JV-1-40, JV-1-41, JV-1-42, JV-1-43, JV-1-62, JV-1-63,MZ-4-71, MZ-4-169, MZ-4-181, MZ-4-243, MZ-5-78,MZ-5-156, MZ-5-192, MZ-6-55, [Ac-Tyr1, D-Arg2]GHRH(1–29)-NH2.
Biological functionsGHRH receptor mRNA is expressed in several organs,especially in the adrenal, digestive tract, and kidney. Theprimary function of GHRH is to stimulate GH synthesisand release from the anterior pituitary somatotrophs.GHRH activates cell proliferation, cell differentiation,and growth of somatotrophs, and is also involved inthe modulation of appetite and feeding behavior, the regulation of sleeping, the control of jejunal motility, and theincrease in leptin levels in modest obesity .
Clinical implicationsMutations in the GHRH gene have never beendescribed. A single base change in the GHRH-R gene inhuman somatotropinoma confers hypersensitivity toGHRH binding. Pit-1 mutation inducing the low geneexpression of GHRH-R can lead to the development ofdwarfism.
DescriptionGHRH is expressed and secreted from the hypothalamicneurons of the arcuate nucleus (ARC). GHRH stimulatesthe release of growth hormone (GH) in the anteriorpituitary. In 1982, three isoforms of GHRH(1–37, 1–40, 1–44 aaresidues) were initially isolated from human pancreatictumors that caused acromegaly, and the latter two werefound in the human hypothalamus. The aa sequence ofGHRH was also identified in various vertebrates fromrodents to fish, including a protochordate. In nonmammalian vertebrates, GHRH-like peptide (pituitary adenylate cyclase-activating polypeptide (PACAP)-relatedpeptide in mammals) was first isolated like GHRH,although the GHRH-like peptide had less activity onGH release. Later, actual GHRH, which was more phylogenetically and structurally similar to mammalianGHRH and showed GH-releasing activity, was isolatedin nonmammalian vertebrates.
UsesHuman growth hormone-releasing factor (Growth Hormone Releasing Factor human) is a hypothalamic polypeptide and stimulates GH production and release by binding to the GHRH Receptor (GHRHR) on cells in the anterior pituitary[1].
Clinical UseSermorelin, a functional peptide fragment of GHRH(1–29), has been used in the diagnosis and treatment ofchildren with idiopathic growth hormone deficiency. Tesamorelin, a stabilized synthetic peptide analog ofGHRH(1–44), received US Food and Drug Administration approval in 2010 for the treatment of lipodystrophyin HIV patients under highly active antiretroviral therapy, and was investigated for effects on certain cognitivefunctions in adults with cognitive impairment as well ashealthy older adults.
DescriptionGrowth Hormone Releasing Hormone Human Synthetic is a single, non-glycosylated, polypeptide chain containing 29 amino acids and having a molecular mass of 3358.9 Dalton.
Corresponds to the amino-terminal segment of the naturally occurring human growth hormone-releasing hormone consisting of 44 amino acid residues.
The GHRH is purified by proprietary chromatographic techniques.
BackgroundGrowth-hormone-releasing hormone (GHRH), also known as growth-hormone-releasing factor (GRF or GHRF) or somatocrinin, is a 44-amino acidpeptide hormoneproduced in the arcuate nucleusof the hypothalamus.
GHRH is released from neurosecretory nerve terminals of these arcuate neurons, and is carried by the hypothalamo-hypophysial portal circulation to the anterior pituitary glandwhere it stimulates growth hormone(GH) secretion. GHRH also stimulates the production of GH. GHRH is released in a pulsatile manner, stimulating similar pulsatile release of GH. In addition, GHRH also promotes slow-wave sleepdirectly.
References[1] Fridlyand LE, et al.Growth Hormone-Releasing Hormone in Diabetes.Front Endocrinol (Lausanne). 2016 Oct 10;7:129. eCollection 2016. DOI:10.3389/fendo.2016.00129

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