產(chǎn)品說明
APJ受體的內(nèi)源性配體
該產(chǎn)品包含在以下化合物庫中:
質(zhì)量控制
化學(xué)性質(zhì)
| CAS號 | 217082-58-1 | ? | ? |
| 別名 |
| 分子式 | C69H111N23O16S | 分子量 | 1550.8 |
| 溶解性 | >155.1mg/ml in DMSO | 儲存條件 | Store at -20° |
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實驗操作
| 細胞實驗[2]： |
| 細胞系 | 血管平滑肌細胞（VSMCs） |
| 溶解方法 | 可溶于DMSO。若獲取更高濃度的溶液，可在37℃下孵育10分鐘，隨后在超聲波浴中搖勻。-20℃以下可儲存數(shù)月。 |
| 反應(yīng)時間 | |
| 應(yīng)用 | Apelin-13通過誘導(dǎo)磷酸肌醇3激酶（PI3K）/Akt信號轉(zhuǎn)導(dǎo)途徑，促進VSMC增殖。Apelin-13（0.5-4 μM）以劑量和時間依賴的方式促進磷酸化PI3K和磷酸化Akt的表達。Apelin-13通過PI3K/Akt信號傳導(dǎo)通路促進VSMC增殖。 |
| 動物實驗[3]： |
| 動物模型 | Wistar大鼠，心肌I/R損傷嚙齒動物（小鼠和大鼠）模型 |
| 劑量 | 腦室內(nèi)（ICV）給藥，靜脈注射（IV）10 nmol |
| 注意事項 | 由于實驗環(huán)境的不同，實際溶解度可能與理論值略有不同，請測試室內(nèi)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. |
產(chǎn)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.
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