Apelin-13

￥546 1EA 起订

上海更新日期：2019-12-18

上海伟寰生物科技有限公司

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产品详情:

英文名称：: Apelin-13

货号：: C3633

规格：: 1mg/5mg/10mg/25mg

产品说明

APJ受体的内源性配体

该产品包含在以下化合物库中:

质量控制

纯度 = 98.60%

化学性质

CAS号	217082-58-1
别名
分子式	C₆₉H₁₁₁N₂₃O₁₆S	分子量	1550.8
溶解性	>155.1mg/ml in DMSO	储存条件	Store at -20°

实验操作

细胞实验[2]：
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。
反应时间
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[3]：
动物模型	Wistar大鼠，心肌I/R损伤啮齿动物（小鼠和大鼠）模型
剂量	脑室内（ICV）给药，静脉注射（IV）10 nmol
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.][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.][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.][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.][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.

产品描述

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.

温馨提示：不可用于临床治疗。

Apelin-13;生物化学