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140703-51-1

140703-51-1 structure
140703-51-1 structure
  • Name: Hexarelin
  • Chemical Name: Hexarelin
  • CAS Number: 140703-51-1
  • Molecular Formula: C47H58N12O6
  • Molecular Weight: 887.04000
  • Catalog: Biochemical Peptide
  • Create Date: 2018-02-11 08:00:00
  • Modify Date: 2024-01-02 12:36:18
  • 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.
Name Hexarelin
Synonyms MFCD00671439
M.W. 887.04 C47H58N12O6
L-Histidyl-2-methyl-D-tryptophyl-L-alanyl-L-tryptophyl-D-phenylalanyl-L-lysinamide
Hexarelin
HIS-D-2-METHYL-TRP-D-PHE-LYS-NH2
Examorelin
GROWTH HORMONE RELEASING HEXAPEPTIDE
HIS-D-2-ME-TRP-ALA-TRP-D-PHE-LYS-NH2
L-Lysinamide, L-histidyl-2-methyl-D-tryptophyl-L-alanyl-L-tryptophyl-D-phenylalanyl-
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.
Related Catalog
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].
Cell Assay 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].
Animal Admin Rats[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.
References

[1]. Huang J, et al. The Growth Hormone Secretagogue Hexarelin Protects Rat Cardiomyocytes From in vivo Ischemia/Reperfusion Injury Through Interleukin-1 Signaling Pathway. Int Heart J. 2017 Apr 6;58(2):257-263.

[2]. Zhao Y, et al. Hexarelin Protects Rodent Pancreatic Β-Cells Function from Cytotoxic Effects of Streptozotocin Involving Mitochondrial Signalling Pathways In Vivo and In Vitro. PLoS One. 2016 Feb 26;11(2):e0149730.
Density 1.322 g/cm3
Boiling Point 1403.6ºC at 760 mmHg
Molecular Formula C47H58N12O6
Molecular Weight 887.04000
Flash Point 802.7ºC
Exact Mass 886.46000
PSA 300.89000
LogP 5.39220
Vapour Pressure 0mmHg at 25°C
Index of Refraction 1.66
Storage condition ?20°C
Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR NONH for all modes of transport
RTECS OL4683333

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