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Apelin-13
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Apelin-13图片
CAS NO:217082-58-1
规格:98%
分子量:1550.8
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
endogenous ligand of the APJ receptor
CAS:217082-58-1
分子式:C69H111N23O16S
分子量:1550.8
纯度:98%
存储:Store at -20°C

Background:

IC50: 0.37 nM for GPCR


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.


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].


Clinical trial: Previous clinical study showed that intrabrachial infusions of (Pyr1)apelin-13, acetylcholine, and sodium nitroprusside could cause forearm vasodilatation in patients and control subjects. Systemic infusions of (Pyr1)apelin-13 was able to increase cardiac index and lower mean arterial pressure and peripheral vascular resistance in patients and healthy control subjects but increased heart rate only in control subjects [3].


参考文献:
[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.