[CAS NO. ]  Apelin-13 TFA

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PRODUCTS SPECIFICATIONS

Catalog
HY-P1944A
Brand
MCE
CAS
-

DESCRIPTION

Overview

MDL-
Molecular Weight1664.85
Molecular FormulaC71H112F3N23O18S
SMILES-

For research use only. We do not sell to patients.


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

In Vitro:

H 2 O : 50 mg/mL ( 30.03 mM ; Need ultrasonic)

Preparing
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
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: PBS

    Solubility: 100 mg/mL (60.07 mM); Clear solution; Need ultrasonic

* All of the co-solvents are available by MCE.