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[CAS NO. ] Apelin-13 TFA
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-P1944A |
| Brand: | MCE |
| CAS: | - |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 1664.85 |
| Molecular Formula | C71H112F3N23O18S |
| SMILES | - |
3 Publications Citing Use of MCE
Summary
Apelin-13 TFA is an endogenous ligand for the G-protein coupled receptor angiotensin II protein J (APJ) , activating this G protein-coupled receptor with an EC 50 value of 0.37 nM. Apelin-13 TFA has vasodilatory and antihypertensive effects. Apelin-13 TFA also can be used for researching type 2 diabetes and metabolic syndrome [1] [2] [3] .
IC50 & Target
IC 50 : 0.37 nM (APJ) [1]
In Vivo
Apelin-13 (200 µg/kg; IP, daily for 4 weeks) improves cardiac function, improves insulin resistance, improves lipid metabolism, significantly decreases TNF-α and leptin on serum, induces the expression of Apelin-12 in serum and markedly elevates GLUT4 and p-AMPKα2 levels
[2]
.
Apelin-13 (10 and 100 μM; ICV, single dosage) increases the spontaneous discharges in the majority of pallidal neurons
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | 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] |
| Dosage: | 200 µg/kg |
| Administration: | IP, daily for 4 weeks |
| Result: | Significantly decreased heart rate; lowered the levels of fasting plasma glucose (FPG), fasting insulin (FINS) and homeostasis model assessment for insulin resistancey (HOMA-IR); decreased serum levels of total cholesterol (TC), triglyceride (TG) and low density lipoprotein-cholesterol (LDL-C) and increased high density lipoprotein-cholesterol (HDL-C); decreased NO level, cNOS activity, TNF-α and leptin in serum; induced the expression of Apelin-12. |
| Animal Model: | Adult Wistar rats (SPF, 8-10 weeks, 240-280 g) [4] |
| Dosage: | 10 and 100 μM |
| Administration: | ICV, single dosage |
| Result: | Increased the spontaneous discharges in the majority of pallidal neurons. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01590108 | Imperial College London |
Idiopathic Pulmonary Arterial Hypertension
|
March 2012 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Sealed storage, away from moisture
| Powder | -80°C | 2 years |
|---|---|---|
| -20°C | 1 year |
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 50 mg/mL ( 30.03 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (60.07 mM); Clear solution; Need ultrasonic
References
- [1] Tatemoto, K., et al. Isolation and characterizaton of a novel endogenous peptide ligand for the human APJ receptor. Biochemical and Biophysical Research Communications 251, 471-476 (1998).
- [2] Li M,et al. 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] Yamaleyeva LM, et al. Apelin-13 in blood pressure regulation and cardiovascular disease. Curr Opin Nephrol Hypertens. 2016 Sep;25(5):396-403.
- [4] Wang Y, et al. Apelin-13 regulates electrical activity in the globus pallidus and induces postural changes in rats. Neural Regen Res. 2021 Nov;16(11):2264-2268.
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