Apelin-13 TFA is an endogenous ligand of the G protein-coupled receptor angiotensin II protein J (APJ), and its EC 50 value for activating G protein-coupled receptors is 0.37 nM. Apelin-13 TFA has vasodilatory and antihypertensive effects. Apelin-13 TFA can also be used in research on type 2 diabetes and metabolic syndrome.

Physicochemical Properties

Molecular Formula	C71H112F3N23O18S
Molecular Weight	1664.85
Related CAS #	Apelin-13;217082-58-1
Appearance	White to off-white solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	IC50: 0.37 nM (APJ)[1]
ln Vivo	Apelin-13 (200 μg/kg; IP, once day for 4 weeks) dramatically lowers serum levels of TNF-α and leptin, enhances lipid metabolism, strengthens cardiac function, and reduces insulin resistance. increases the levels of GLUT4 and p-AMPKα2 and stimulates the expression of Apelin-12 in serum[2]. ?Most pallidal neurons exhibit an increase in spontaneous discharges when exposed to a single dosage of Apelin-13 (10 and 100 μM; ICV)[4].
Animal Protocol	Animal/Disease Models: Goto-Kakizaki (GK) rats (12 weeks old; 240-280 g; fed with a high-fat diet: 66.5% standard chow, 10% lard, 20% sucrose, 2.5% cholesterol and 1% pig bile salt)[2] Doses: 200 µg/kg Route of Administration: IP, daily for 4 weeks Experimental Results: Dramatically diminished heart rate; lowered the levels of fasting plasma glucose (FPG), fasting insulin (FINS) and homeostasis model assessment for insulin resistance (HOMA-IR); diminished serum levels of total cholesterol (TC), triglyceride (TG) and low density lipoprotein-cholesterol (LDL-C) and increased high density lipoprotein-cholesterol (HDL-C); diminished NO level, cNOS activity, TNF-α and leptin in serum; induced the expression of Apelin-12. Animal/Disease Models: Adult Wistar rats (SPF, 8-10 weeks, 240-280 g)[4] Doses: 10 and 100 μM Route of Administration: ICV, single dosage Experimental Results: Increased the spontaneous discharges in the majority of pallidal neurons.
References	[1]. Isolation and characterizaton of a novel endogenous peptide ligand for the human APJ receptor. Biochemical and Biophysical Research Communications 251, 471-476 (1998). [2]. Apelin 13 ameliorates metabolic and cardiovascular disorders in a rat model of type 2 diabetes with a high fat diet. Mol Med Rep. 2018 Dec;18(6):5784-5790. [3]. Apelin-13 in blood pressure regulation and cardiovascular disease. Curr Opin Nephrol Hypertens. 2016 Sep;25(5):396-403. [4]. Apelin-13 regulates electrical activity in the globus pallidus and induces postural changes in rats. Neural Regen Res. 2021 Nov;16(11):2264-2268.

Solubility Data

Solubility (In Vitro)	H2O :~50 mg/mL (~30.03 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 100 mg/mL (60.07 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.6007 mL	3.0033 mL	6.0065 mL
	5 mM	0.1201 mL	0.6007 mL	1.2013 mL
	10 mM	0.0601 mL	0.3003 mL	0.6007 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.