1. GPCR/G Protein
  2. GHSR

Examorelin (Synonyms: Hexarelin; His-D-2-ME-Trp-Ala-Trp-d-Phe-Lys-NH2; H{D-2-ME-TRP}AW{d-PHE}K-NH2)

Cat. No.: HY-19235
Handling Instructions

Examorelin, a synthetic growth hormone-releasing peptide, has been proven to possess cardioprotective actions through its binding to the growth hormone secretagogue receptor (GHSR) 1a and the non-GHSR receptor CD36.

For research use only. We do not sell to patients.
Examorelin Chemical Structure

Examorelin Chemical Structure

CAS No. : 140703-51-1

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  • Biological Activity

  • Protocol

  • Technical Information

  • References

Description

Examorelin, a synthetic growth hormone-releasing peptide, has been proven to possess cardioprotective actions through its binding to the growth hormone secretagogue receptor (GHSR) 1a and the non-GHSR receptor CD36.

IC50 & Target

GHSR[1]

In Vitro

Cultured MIN6 cells are incubated with serum-free medium (SFM) (control), 1 μM Examorelin (Hex), 1 mM Streptozotocin (STZ) alone or STZ followed by Examorelin for 6 hours. The viability of MIN6 is significantly affected by different treatments of the cells (F(3, 36)=5.244,P<0.01) . MIN6 cells treated with STZ followed by Examorelin receive a great increase in the cell viability (105.3% of control, P<0.01) as compared with those treated with STZ alone[2].

In Vivo

Examorelin (Hexarelin) treatment improves cardiac systolic function, decreases malondialdehyde production, and increases the number of surviving cardiomyocytes. The beneficial effects of Examorelin treatment are slightly superior to those of equimolar ghrelin treatment. Examorelin also induces down-regulation of IL-1β expression and up-regulation of IL-1Ra expression in I/R myocardium, which could be neutralized by the GHSR antagonist (D-Lys3)-GHRP-6. Examorelin protects in vivo cardiomyocytes from I/R injury partly by modification of the IL-1 signaling pathway through the activation of cardiac GHSR1a receptors[1]. The effect of Examorelin (100 μg/kg) in STZ-induced diabetic rats is examined. STZ-injection dramatically increased blood glucose levels in rats whereas Examorelin (Hex) treatment diminished the effect of STZ. Plasma insulin levels of rats are measured under both fasting and fed conditions respectively. Different treatment exerted significant effects on fasting insulin level (F(3, 28)=7.472, P<0.01) . The Examorelin alone increases the plasma insulin (P<0.05) whereas the STZ dramatically decreases it (P<0.001). STZ+Examorelin -treated rats show an increased insulin level (P<0.001). Similar to fasting insulin level, fed insulin level (Ftreatment (3, 28)=61.89, P<0.001) are significantly increased in Examorelin-treated rats (P<0.001) and reduced in STZ-treated rats. Furthermore, the Examorelin also ameliorates STZ-induced decrease in fed plasma insulin level[2].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.1273 mL 5.6367 mL 11.2734 mL
5 mM 0.2255 mL 1.1273 mL 2.2547 mL
10 mM 0.1127 mL 0.5637 mL 1.1273 mL
Cell Assay
[2]

MIN6 and α-TC6 cells are seeded in 96-well plates and cultured in the presence or absence of Examorelin (1 μM) and STZ (1 mM) for 0.5, 1, 2, 4, and 6 hours. After the treatment, cells are replaced in fresh SFM and the number of viable cells is quantified using CellTiter 96 Aqueous One Solution Cell Proliferation Assay , which contains the tetrazolium compound MTS. Cell viability is determined by measuring absorbance at 490 nm with a microplate reader and expressed as a percentage relative to control cells[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Examorelin (Hex) is prepared in vehicle (saline) (Rat)[2].

Rat[2]
Experiments are performed in male Wistar rats (180–200 g). Rats are housed separately under standard housing conditions (lights on from 06:00 to 18:00, temperature 22±2°C) and have access to food and water ad libitum. A single intraperitoneal injection of STZ dissolved in a 0.1 mol/L citrate buffer (pH 4.5) is used at a dose of 65 mg/kg body weight. Age-matched control rats receive an equal volume of vehicle (sodium citrate buffer). Four weeks after STZ or vehicle injection, rats are randomly assigned to 4 groups (n=16/group) according to the treatment: rats with vehicle then saline for 2 weeks (control group); or 100 μg/kg Examorelin for 2 weeks (Examorelin treated group); STZ-treated rats then saline for 2 weeks (STZ treated group); or 100 μg/kg Examorelin for 2 weeks (STZ+Examorelin treated group). Saline and Examorelin are intraperitoneally injected daily.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

887.04

Formula

C₄₇H₅₈N₁₂O₆

CAS No.

140703-51-1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Examorelin
Cat. No.:
HY-19235
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