217082-58-1 Usage
Description
GLN-ARG-PRO-ARG-LEU-SER-HIS-LYS-GLY-PRO-MET-PRO-PHE is a peptide sequence consisting of 12 amino acids. It is derived from the apelin gene, which encodes a pre-proprotein that is processed to generate bioactive peptides, including apelin-13. Apelin-13 is an endogenous ligand of the APJ receptor and plays crucial roles in regulating various physiological functions.
Uses
Used in Pharmaceutical Applications:
GLN-ARG-PRO-ARG-LEU-SER-HIS-LYS-GLY-PRO-MET-PRO-PHE, as apelin-13, is used as a therapeutic agent for various medical conditions due to its regulatory effects on cardiovascular function, fluid homeostasis, hypertension, and insulin sensitivity.
Used in Research Applications:
GLN-ARG-PRO-ARG-LEU-SER-HIS-LYS-GLY-PRO-MET-PRO-PHE is used in scientific research to study the progression of diabetic nephropathy (DN) by inducing podocyte dysfunction and to examine the effects of apelin on myocardial infarction (MI) injury and underlying mechanisms.
Used in Drug Delivery Systems:
In the field of drug delivery, GLN-ARG-PRO-ARG-LEU-SER-HIS-LYS-GLY-PRO-MET-PRO-PHE may be utilized to develop novel drug delivery systems to enhance the efficacy and bioavailability of apelin-13 for targeted therapeutic applications.
Used in the Pharmaceutical Industry:
GLN-ARG-PRO-ARG-LEU-SER-HIS-LYS-GLY-PRO-MET-PRO-PHE is used as a bioactive peptide in the pharmaceutical industry for the development of drugs targeting cardiovascular diseases, fluid homeostasis disorders, and metabolic conditions such as diabetes.
Used in the Biotechnology Industry:
GLN-ARG-PRO-ARG-LEU-SER-HIS-LYS-GLY-PRO-MET-PRO-PHE is used as a key component in the biotechnology industry for the development of innovative therapies and drug delivery systems, focusing on the potential applications of apelin-13 in treating various medical conditions.
Biological Activity
apelin-13 is an endogenous ligand of the apj receptor.the apelin receptor apj, one of a group of g-proteincoupled receptors (gpcr), have recently been paired with their cognate peptide ligands using ‘‘reverse pharmacology’’, and functional evidence suggests a role for this receptor in the regulation of cardiovascular function, fluid homeostasis, and as a coreceptor for hiv infection.
Biochem/physiol Actions
Apelin plays physiological roles in the cytoprotection of many internal organs. It is used to treat insulin resistance and hypertension, but it may also can act as a negative factor. Apelin also regulates cardiovascular diseases.
in vitro
apelin-13 was identified as an endogenous ligand of the apj receptor, which could activate this g protein-coupled receptor with an ec50 value of 0.37 nm. in addition, the ec50 values for apelin-17 and apelin-36 have been found to be 2.5 and 20 nm, respectively [1].
in vivo
in a previous study, urethane anaesthetised, paralysed and ventilated male sd rats were used to investigate the action of apelin-13 directly microinjected into the nucleus tractus solitarius (nts) and the rostral ventrolateral medulla (rvlm) on arterial pressure and phrenic nerve activity. results showed that apelin-13 microinjections into the nts led to either apnea or decreased phrenic nerve discharge amplitude by up to 30%. in the rvlm, apelin-13 caused increase in phrenic nerve discharge amplitude depending on the exact site of injection [2].
IC 50
0.37 nm for gpcr
references
[1] lee, d. k.,cheng, r.,nguyen, t., et al. characterization of apelin, the ligand for the apj receptor. journal of neurochemistry 74, 34-41 (2000).[2] seyedabadi m, goodchild ak, pilowsky pm. site-specific effects of apelin-13 in the rat medulla oblongata on arterial pressure and respiration. auton neurosci. 2002 oct 31;101(1-2):32-8.[3] a g japp, n l cruden, g barnes, n van gemeren, j mathews, j adamson, n r johnston, m a denvir, i l megson, a d flapan, d e newby. acute cardiovascular effects of apelin in humans: potential role in patients with chronic heart failure. circulation 2010 april 27, 121 (16): 1818-27.
Check Digit Verification of cas no
The CAS Registry Mumber 217082-58-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,1,7,0,8 and 2 respectively; the second part has 2 digits, 5 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 217082-58:
(8*2)+(7*1)+(6*7)+(5*0)+(4*8)+(3*2)+(2*5)+(1*8)=121
121 % 10 = 1
So 217082-58-1 is a valid CAS Registry Number.
217082-58-1Relevant articles and documents
DERIVATIVES COMPRISING AN APELIN ANALOGUE AND USES THEREOF
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Page/Page column 33-35; 39, (2019/12/25)
The present invention relates to derivatives comprising an apelin analogue; wherein the apelin analogue comprises two amino acids having a sulphur atom in the side chain, wherein said two amino acids are covalently linked via a methylene bridge. The invention also relates to the pharmaceutical use of the derivatives, preferably in the treatment of all forms of cardiovascular disease.
