217082-60-5 Usage
Description
PYR-ARG-PRO-ARG-LEU-SER-HIS-LYS-GLY-PRO-MET-PRO-PHE-OH, also known as (Glp1)-Apelin-13, is a bioactive peptide derived from the apelin gene. It is a pyroglutamylated form of apelin-13, where the N-terminal glutamine residue is cyclized to pyroglutamic acid. PYR-ARG-PRO-ARG-LEU-SER-HIS-LYS-GLY-PRO-MET-PRO-PHE-OH acts as a potent agonist of the APJ receptor, a G protein-coupled receptor, and is the major apelin isoform found in the plasma of healthy human subjects. It exhibits vasoconstrictor and antipyretic effects both in vitro and in vivo.
Uses
Used in Pharmaceutical Applications:
(Glp1)-Apelin-13 is used as a therapeutic agent for various conditions due to its potent agonist activity on the APJ receptor. Its vasoconstrictor and antipyretic effects make it a candidate for the treatment of cardiovascular and temperature regulation disorders.
Used in Research Applications:
In the field of research, (Glp1)-Apelin-13 is utilized as a tool to study the APJ receptor's role in various physiological processes. It helps researchers understand the receptor's involvement in cardiovascular function, body temperature regulation, and other related pathways.
Used in Drug Development:
(Glp1)-Apelin-13 serves as a lead compound in the development of new drugs targeting the APJ receptor. Its potent agonist activity and understanding of its effects on the receptor can guide the design and synthesis of novel therapeutic agents for treating related conditions.
Used in Diagnostic Applications:
(Glp1)-Apelin-13 can be employed as a diagnostic marker for conditions related to the APJ receptor's dysfunction. Measuring the levels of this peptide in plasma or other biological samples can provide insights into the receptor's activity and help in the diagnosis of associated disorders.
Used in Application Industry:
PYR-ARG-PRO-ARG-LEU-SER-HIS-LYS-GLY-PRO-MET-PRO-PHE-OH is used as a bioactive peptide in the pharmaceutical and biotechnology industry for the development of therapeutic agents, research tools, and diagnostic markers targeting the APJ receptor and its associated pathways.
Check Digit Verification of cas no
The CAS Registry Mumber 217082-60-5 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, 6 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 217082-60:
(8*2)+(7*1)+(6*7)+(5*0)+(4*8)+(3*2)+(2*6)+(1*0)=115
115 % 10 = 5
So 217082-60-5 is a valid CAS Registry Number.
217082-60-5Relevant articles and documents
Linking (Pyr)1apelin-13 pharmacokinetics to efficacy: Stabilization and measurement of a high clearance peptide in rodents
Onorato, Joelle M.,Xu, Carrie,Chen, Xue-Qing,Rose, Anne V.,Generaux, Claudia,Lentz, Kimberley,Shipkova, Petia,Arthur, Susan,Hennan, James K.,Haskell, Roy,Myers, Michael C.,Lawrence, R. Michael,Finlay, Heather J.,Basso, Michael,Bostwick, Jeffrey,Fernando, Gayani,Garcia, Ricardo,Hellings, Samuel,Hsu, Mei-Yin,Zhang, Rongan,Zhao, Lei,Gargalovic, Peter
, p. 41 - 50 (2019)
Apelin, the endogenous ligand for the APJ receptor, has generated interest due to its beneficial effects on the cardiovascular system. Synthesized as a 77 amino acid preproprotein, apelin is post-translationally cleaved to a series of shorter peptides. Though (Pyr)1apelin-13 represents the major circulating form in plasma, it is highly susceptible to proteolytic degradation and has an extremely short half-life, making it challenging to quantify. Literature reports of apelin levels in rodents have historically been determined with commercial ELISA kits which suffer from a lack of selectivity, recognizing a range of active and inactive isoforms of apelin peptide. (Pyr)1apelin-13 has demonstrated beneficial hemodynamic effects in humans, and we wished to evaluate if similar effects could be measured in pre-clinical models. Despite development of a highly selective LC/MS/MS method, in rodent studies where (Pyr)1apelin-13 was administered exogenously the peptide was not detectable until a detailed stabilization protocol was implemented during blood collection. Further, the inherent high clearance of (Pyr)1apelin-13 required an extended release delivery system to enable chronic dosing. The ability to deliver sustained doses and stabilize (Pyr)1apelin-13 in plasma allowed us to demonstrate for the first time the link between systemic concentration of apelin and its pharmacological effects in animal models.
