Apelin-13

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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。

CAS NO:

217082-58-1

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

化学性质

Storage	Store at -20°C
M.Wt	1550.8
Cas No.	217082-58-1
Formula	C₆₉H₁₁₁N₂₃O₁₆S
Solubility	≥155.1 mg/mL in DMSO; ≥14.67 mg/mL in EtOH; ≥29.4 mg/mL in H2O
Chemical Name	L-glutaminyl-L-arginyl-L-prolyl-L-arginyl-L-leucyl-L-seryl-L-histidyl-L-lysylglycyl-L-prolyl-L-methionyl-L-prolyl-L-phenylalanine
Canonical SMILES	O=C([C@H](CCSC)NC(C1N(C(CNC([C@H](CCCCN)NC([C@@H](NC([C@H](CO)NC([C@H](CC(C)C)NC([C@H](CCCNC(N)=N)NC([C@H]2N(C([C@@H](NC([C@@H](N)CCC(N)=O)=O)CCCNC(N)=N)=O)CCC2)=O)=O)=O)=O)CC3=CN=CN3)=O)=O)=O)CCC1)=O)N4[C@H](C(N[C@H](C(O)=O)CC5=CC=CC=C5)=O)CCC4
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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].

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.

试验操作

细胞实验 [1]:
细胞系	血管平滑肌细胞（VSMCs）
溶解方法	可溶于DMSO。若获取更高浓度的溶液，可在37℃下孵育10分钟，随后在超声波浴中摇匀。-20℃以下可储存数月。
反应条件	24 h
应用	Apelin-13通过诱导磷酸肌醇3激酶（PI3K）/Akt信号转导途径，促进VSMC增殖。Apelin-13（0.5-4 μM）以剂量和时间依赖的方式促进磷酸化PI3K和磷酸化Akt的表达。Apelin-13通过PI3K/Akt信号传导通路促进VSMC增殖。
动物实验 [2-4]:
动物模型	Wistar大鼠，心肌I/R损伤啮齿动物（小鼠和大鼠）模型
给药剂量	脑室内（ICV）给药，静脉注射（IV）10 nmol
应用	在大鼠中，Apelin-13对食物摄入影响不大，但在1小时时，Apelin-13以剂量依赖性方式增加饮酒行为和摄水量。Apelin-13（10 nmol）增加了水分摄入。Apelin-13（10 nmol）在30分钟时显著增加血浆ACTH和皮质酮含量，降低血浆催乳素、LH和FSH含量。在心肌I/R损伤啮齿动物（小鼠和大鼠）模型中，Apelin-13使梗死面积减少43.1％和32.7％。脑室内（ICV）注射1和3 nmol的apelin-13，导致进食和禁食大鼠的食物摄入量降低。
注意事项	由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。
References: [1]. Liu C, Su T, Li F, et al. PI3K/Akt signaling transduction pathway is involved in rat vascular smooth muscle cell proliferation induced by apelin-13[J]. Acta Biochim Biophys Sin, 2010, 42(6): 396-402. [2].Taheri S, Murphy K, Cohen M, et al. The effects of centrally administered apelin-13 on food intake, water intake and pituitary hormone release in rats[J]. Biochemical and biophysical research communications, 2002, 291(5): 1208-1212. [3].Simpkin J C, Yellon D M, Davidson S M, et al. Apelin-13 and apelin-36 exhibit direct cardioprotective activity against ischemiareperfusion injury[J]. Basic research in cardiology, 2007, 102(6): 518. [4]. Sunter D, Hewson A K, Dickson S L. Intracerebroventricular injection of apelin-13 reduces food intake in the rat[J]. Neuroscience letters, 2003, 353(1): 1-4.