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
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。