Apelin-13 |
Katalog-Nr.GC10284 |
Apelin-13 ist ein Peptid, das als Ligand des G-Protein-gekoppelten Rezeptors APJ bekannt ist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 217082-58-1
Sample solution is provided at 25 µL, 10mM.
Apelin-13 is a peptide known as the ligand of the G-protein-coupled receptor APJ. [1]. Apelin-13 activated this G protein-coupled receptor with an EC50 value of 0.37 nM [2]. Apelin has been shown to be involved in the regulation of cardiovascular and fluid homeostasis, food intake, cell proliferation, and angiogenesis [1].
Apelin-13 was shown to inhibit insulin secretion stimulated by high glucose concentrations (10 mM) or potentiated by GLP-1 in INS-1 cells [3]. Apelin-13 at 200 nM can enhance H9c2 cell proliferation, which is mediated by the ERK1/2 and Akt signaling pathway [4].
Apelin-13 treatment significantly lowers blood glucose and protects HFD mice from hyperinsulinemia [5]. There are some contradictory reports about the effects of apelin-13/APJ on hypertension. Intraperitoneally administered Apelin-13 reduces blood pressure in hypertensive rats by inhibiting renin-angiotensin system [6]. Chronic infusion of apelin-13 into the paraventricular nucleus induces hypertension through increasing the levels of plasma norepinephrine and arginine vasopressin in normotensive rats [7].
References:
[1]. Castan-Laurell I, Dray C, AttanÉ C, et al. Apelin, diabetes, and obesity[J]. Endocrine, 2011, 40(1): 1-9.
[2]. Tatemoto K, Hosoya M, Habata Y, et al. Isolation and characterization of a novel endogenous peptide ligand for the human APJ receptor[J]. Biochemical and biophysical research communications, 1998, 251(2): 471-476.
[3]. Guo L, Li Q, Wang W, et al. Apelin inhibits insulin secretion in pancreatic β-cells by activation of PI3-kinase-phosphodiesterase 3B[J]. Endocrine research, 2009, 34(4): 142-154.
[4]. Yin L, Zhang P, Li C, et al. Apelin?13 promotes cell proliferation in the H9c2 cardiomyoblast cell line by triggering extracellular signal?regulated kinase 1/2 and protein kinase B phosphorylation[J]. Molecular Medicine Reports, 2018, 17(1): 447-451.
[5]. AttanÉ C, Foussal C, Le Gonidec S, et al. Apelin treatment increases complete Fatty Acid oxidation, mitochondrial oxidative capacity, and biogenesis in muscle of insulin-resistant mice[J]. Diabetes, 2012, 61(2): 310-320.
[6]. Akc?lar R, Turgut S, Caner V, et al. Apelin effects on blood pressure and RAS in DOCA-salt-induced hypertensive rats[J]. Clinical and Experimental Hypertension, 2013, 35(7): 550-557.
[7]. Zhang F, Sun H J, Xiong X Q, et al. Apelin©\13 and APJ in paraventricular nucleus contribute to hypertension via sympathetic activation and vasopressin release in spontaneously hypertensive rats[J]. Acta physiologica, 2014, 212(1): 17-27.
Cell experiment [1]: | |
Cell lines |
H9c2 cells |
Preparation Method |
Cells were allowed to reach 80% confluence in complete DMEM and were incubated for an additional 24 h in serum-free medium prior to experimental treatments. Following this, H9c2 cells were treated with 0, 5, 25, 50, 100, 200, 400, 600, 800 or 1,000 nM Apelin-13 for 24 h |
Reaction Conditions |
0, 5, 25, 50, 100, 200, 400, 600, 800 or 1,000 nM for 24 hours |
Applications |
Apelin-13 treatment increased the percentage cell viability compared with the baseline constitutive release over a range of physiological extracellular concentrations from 50 to 600 nM, with a maximal effect at 200 nM. |
Animal experiment [2]: | |
Animal models |
male Sprague-Dawley rats |
Preparation Method |
Rats were injected with a 0.9% equivolume saline control before peptide injection. Apelin-13 was dissolved as a stock solution of 40 µg/ml in 0.9% saline and administered intravenously at ∼3-6 µg/kg B.W., i.e., 1-2 µg per 300-g rat. |
Dosage form |
Intravenous injection, 1-2 µg per 300-g |
Applications |
An apelin-13 dose of 1 µg/300 g B.W. elicited an immediate change in blood pressure of -10.0 ± 1.9 mm Hg systolic and -13.0 ± 2.8 mm Hg diastolic. A 2 µg/300 g B.W. dose elicited immediate blood pressure changes of -9.8 ± 1.2 systolic and -13.2 ± 1.7 mm Hg diastolic. |
References: [1]: Yin L, Zhang P, Li C, et al. Apelin?13 promotes cell proliferation in the H9c2 cardiomyoblast cell line by triggering extracellular signal?regulated kinase 1/2 and protein kinase B phosphorylation[J]. Molecular Medicine Reports, 2018, 17(1): 447-451. |
Cas No. | 217082-58-1 | SDF | |
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 | ||
Formula | C69H111N23O16S | M.Wt | 1550.8 |
Löslichkeit | ≥ 155.1mg/mL in DMSO; 100mg/mL in Water | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 0.6448 mL | 3.2241 mL | 6.4483 mL |
5 mM | 0.129 mL | 0.6448 mL | 1.2897 mL |
10 mM | 0.0645 mL | 0.3224 mL | 0.6448 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5
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