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MedKoo Cat#: 530032 | Name: Examorelin
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Examorelin is a synthetic growth hormone-releasing peptide (GHRP) that stimulates the secretion of growth hormone (GH) from the anterior pituitary. It acts by binding to the ghrelin receptor (GHS-R1a), triggering the release of GH via a mechanism that involves activation of the G protein-coupled receptor pathway and subsequent release of endogenous GH. Examorelin is used in clinical settings to assess growth hormone secretion and has potential applications in growth hormone deficiency treatment.

Chemical Structure

Examorelin
Examorelin
CAS#140703-51-1

Theoretical Analysis

MedKoo Cat#: 530032

Name: Examorelin

CAS#: 140703-51-1

Chemical Formula: C47H58N12O6

Exact Mass: 886.4600

Molecular Weight: 887.06

Elemental Analysis: C, 63.64; H, 6.59; N, 18.95; O, 10.82

Price and Availability

Size Price Availability Quantity
1mg USD 350.00 2 Weeks
5mg USD 850.00 2 Weeks
10mg USD 1,250.00 2 Weeks
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Related CAS #
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Synonym
Hexarelin; Examorelin; Examorelina; Examoreline; Examorelinum; EP-23905; EP23905; EP 23905; MF 6003; MF-6003; MF6003; H-2-Me-WAWFK; His-2-Me-Trp-Ala-Trp-Phe-Lys-NH2; His-(D)-Mrp-Ala-Trp-(D)-Phe-Lys-NH2
IUPAC/Chemical Name
L-Lysinamide, L-histidyl-2-methyl-D-tryptophyl-L-alanyl-L-tryptophyl-D-phenylalanyl-
InChi Key
RVWNMGKSNGWLOL-GIIHNPQRSA-N
InChi Code
InChI=1S/C47H58N12O6/c1-27-34(33-15-7-9-17-37(33)54-27)23-41(58-44(62)35(49)22-31-25-51-26-53-31)45(63)55-28(2)43(61)57-40(21-30-24-52-36-16-8-6-14-32(30)36)47(65)59-39(20-29-12-4-3-5-13-29)46(64)56-38(42(50)60)18-10-11-19-48/h3-9,12-17,24-26,28,35,38-41,52,54H,10-11,18-23,48-49H2,1-2H3,(H2,50,60)(H,51,53)(H,55,63)(H,56,64)(H,57,61)(H,58,62)(H,59,65)/t28-,35-,38-,39+,40-,41+/m0/s1
SMILES Code
NCCCC[C@@H](C(N)=O)NC([C@@H](CC1=CC=CC=C1)NC([C@H](CC2=CNC3=C2C=CC=C3)NC([C@H](C)NC([C@@H](CC4=C(C)NC5=C4C=CC=C5)NC([C@H](CC6=CNC=N6)N)=O)=O)=O)=O)=O
Appearance
Solid powder
Purity
>90% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
A peptide agonist of GHS-R.
In vitro activity:
Ang-II induced cardiomyocyte hypertrophy, oxidative stress, apoptosis and decreased cell survival, all of which were significantly suppressed by hexarelin treatment which also enhanced autophagy in hypertrophic H9C2 cells. Reference: Pharmazie. 2019 Aug 1;74(8):485-491. https://pubmed.ncbi.nlm.nih.gov/31526442/
In vivo activity:
IR-injured and sham mice were subjected to high-field magnetic resonance imaging to assess left ventricular (LV) function, with HEX (hexarelin)-treated mice demonstrating a significant improvement in LV function compared with VEH-treated mice. A significant decrease in interstitial collagen, TGF-β1 expression and myofibroblast differentiation was also seen in the HEX-treated mice after 21 days. HEX treatment shifted the ANS balance towards a parasympathetic predominance; combined with a significant decrease in cardiac troponin-I and TNF-α levels, these findings were suggestive of an anti-inflammatory action on the myocardium mediated via HEX. In this model of IR, HEX appeared to rebalance the deregulated ANS and activate vagal anti-inflammatory pathways to prevent adverse remodelling and LV dysfunction. Reference: Biomed Pharmacother. 2020 Jul;127:110165. https://pubmed.ncbi.nlm.nih.gov/32403043/
Solvent mg/mL mM
Solubility
DMSO 30.0 33.82
DMF 30.0 33.82
Ethanol 5.0 5.64
PBS (pH 7.2) 10.0 11.27
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 887.06 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Meanti R, Rizzi L, Bresciani E, Molteni L, Locatelli V, Coco S, Omeljaniuk RJ, Torsello A. Hexarelin Modulation of MAPK and PI3K/Akt Pathways in Neuro-2A Cells Inhibits Hydrogen Peroxide-Induced Apoptotic Toxicity. Pharmaceuticals (Basel). 2021 May 8;14(5):444. doi: 10.3390/ph14050444. PMID: 34066741; PMCID: PMC8150489. 2. Agbo E, Li MX, Wang YQ, Saahene RO, Massaro J, Tian GZ. Hexarelin protects cardiac H9C2 cells from angiotensin II-induced hypertrophy via the regulation of autophagy. Pharmazie. 2019 Aug 1;74(8):485-491. doi: 10.1691/ph.2019.9324. PMID: 31526442. 3. McDonald H, Peart J, Kurniawan ND, Galloway G, Royce SG, Samuel CS, Chen C. Hexarelin targets neuroinflammatory pathways to preserve cardiac morphology and function in a mouse model of myocardial ischemia-reperfusion. Biomed Pharmacother. 2020 Jul;127:110165. doi: 10.1016/j.biopha.2020.110165. Epub 2020 May 8. PMID: 32403043. 4. Cheng XL, Ding F, Wang DP, Zhou L, Cao JM. Hexarelin attenuates atherosclerosis via inhibiting LOX-1-NF-κB signaling pathway-mediated macrophage ox-LDL uptake in ApoE-/- mice. Peptides. 2019 Nov;121:170122. doi: 10.1016/j.peptides.2019.170122. Epub 2019 Aug 3. PMID: 31386895.
In vitro protocol:
1. Meanti R, Rizzi L, Bresciani E, Molteni L, Locatelli V, Coco S, Omeljaniuk RJ, Torsello A. Hexarelin Modulation of MAPK and PI3K/Akt Pathways in Neuro-2A Cells Inhibits Hydrogen Peroxide-Induced Apoptotic Toxicity. Pharmaceuticals (Basel). 2021 May 8;14(5):444. doi: 10.3390/ph14050444. PMID: 34066741; PMCID: PMC8150489. 2. Agbo E, Li MX, Wang YQ, Saahene RO, Massaro J, Tian GZ. Hexarelin protects cardiac H9C2 cells from angiotensin II-induced hypertrophy via the regulation of autophagy. Pharmazie. 2019 Aug 1;74(8):485-491. doi: 10.1691/ph.2019.9324. PMID: 31526442.
In vivo protocol:
1. McDonald H, Peart J, Kurniawan ND, Galloway G, Royce SG, Samuel CS, Chen C. Hexarelin targets neuroinflammatory pathways to preserve cardiac morphology and function in a mouse model of myocardial ischemia-reperfusion. Biomed Pharmacother. 2020 Jul;127:110165. doi: 10.1016/j.biopha.2020.110165. Epub 2020 May 8. PMID: 32403043. 2. Cheng XL, Ding F, Wang DP, Zhou L, Cao JM. Hexarelin attenuates atherosclerosis via inhibiting LOX-1-NF-κB signaling pathway-mediated macrophage ox-LDL uptake in ApoE-/- mice. Peptides. 2019 Nov;121:170122. doi: 10.1016/j.peptides.2019.170122. Epub 2019 Aug 3. PMID: 31386895.
1: Mao Y, Tokudome T, Kishimoto I, Otani K, Miyazato M, Kangawa K. One dose of oral hexarelin protects chronic cardiac function after myocardial infarction. Peptides. 2014 Jun;56:156-62. doi: 10.1016/j.peptides.2014.04.004. PubMed PMID: 24747279. 2: Mao Y, Tokudome T, Kishimoto I, Otani K, Hosoda H, Nagai C, Minamino N, Miyazato M, Kangawa K. Hexarelin treatment in male ghrelin knockout mice after myocardial infarction. Endocrinology. 2013 Oct;154(10):3847-54. doi: 10.1210/en.2013-1291. PubMed PMID: 23861368. 3: Xu X, Ding F, Pang J, Gao X, Xu RK, Hao W, Cao JM, Chen C. Chronic administration of hexarelin attenuates cardiac fibrosis in the spontaneously hypertensive rat. Am J Physiol Heart Circ Physiol. 2012 Sep 15;303(6):H703-11. doi: 10.1152/ajpheart.00257.2011. PubMed PMID: 22842067. 4: Mosa RM, Zhang Z, Shao R, Deng C, Chen J, Chen C. Implications of ghrelin and hexarelin in diabetes and diabetes-associated heart diseases. Endocrine. 2015 Jun;49(2):307-23. doi: 10.1007/s12020-015-0531-z. Review. PubMed PMID: 25645463. 5: Mao Y, Tokudome T, Kishimoto I. The cardiovascular action of hexarelin. J Geriatr Cardiol. 2014 Sep;11(3):253-8. doi: 10.11909/j.issn.1671-5411.2014.03.007. Review. PubMed PMID: 25278975; PubMed Central PMCID: PMC4178518. 6: Semenistaya E, Zvereva I, Thomas A, Thevis M, Krotov G, Rodchenkov G. Determination of growth hormone releasing peptides metabolites in human urine after nasal administration of GHRP-1, GHRP-2, GHRP-6, Hexarelin, and Ipamorelin. Drug Test Anal. 2015 Oct;7(10):919-25. doi: 10.1002/dta.1787. PubMed PMID: 25869809. 7: Biagini G, Torsello A, Marinelli C, Gualtieri F, Vezzali R, Coco S, Bresciani E, Locatelli V. Beneficial effects of desacyl-ghrelin, hexarelin and EP-80317 in models of status epilepticus. Eur J Pharmacol. 2011 Nov 16;670(1):130-6. doi: 10.1016/j.ejphar.2011.08.020. PubMed PMID: 21914437. 8: Pang J, Xu Q, Xu X, Yin H, Xu R, Guo S, Hao W, Wang L, Chen C, Cao JM. Hexarelin suppresses high lipid diet and vitamin D3-induced atherosclerosis in the rat. Peptides. 2010 Apr;31(4):630-8. doi: 10.1016/j.peptides.2009.11.007. PubMed PMID: 19931584. 9: Yu H, Kim K. Direct nose-to-brain transfer of a growth hormone releasing neuropeptide, hexarelin after intranasal administration to rabbits. Int J Pharm. 2009 Aug 13;378(1-2):73-9. doi: 10.1016/j.ijpharm.2009.05.057. PubMed PMID: 19501141. 10: Bresciani E, Pitsikas N, Tamiazzo L, Luoni M, Bulgarelli I, Cocchi D, Locatelli V, Torsello A. Feeding behavior during long-term hexarelin administration in young and old rats. J Endocrinol Invest. 2008 Jul;31(7):647-52. PubMed PMID: 18787385. 11: Zhao Y, Zhang X, Chen J, Lin C, Shao R, Yan C, Chen C. 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. doi: 10.1371/journal.pone.0149730. PubMed PMID: 26918825; PubMed Central PMCID: PMC4769129. 12: Barlind A, Karlsson N, Åberg ND, Björk-Eriksson T, Blomgren K, Isgaard J. The growth hormone secretagogue hexarelin increases cell proliferation in neurogenic regions of the mouse hippocampus. Growth Horm IGF Res. 2010 Feb;20(1):49-54. doi: 10.1016/j.ghir.2009.09.001. PubMed PMID: 19800825. 13: Xu X, Pang J, Yin H, Li M, Hao W, Chen C, Cao JM. Hexarelin suppresses cardiac fibroblast proliferation and collagen synthesis in rat. Am J Physiol Heart Circ Physiol. 2007 Nov;293(5):H2952-8. PubMed PMID: 17766487. 14: Benso A, Prodam F, Lucatello B, Gramaglia E, Riganti F, Schneider H, van der Lely AJ, Muccioli G, Ghigo E, Broglio F. d-Lys-GHRP-6 does not modify the endocrine response to acylated ghrelin or hexarelin in humans. Neuropeptides. 2007 Feb;41(1):45-9. PubMed PMID: 17112585. 15: Frieboes RM, Antonijevic IA, Held K, Murck H, Pollmächer T, Uhr M, Steiger A. Hexarelin decreases slow-wave sleep and stimulates the secretion of GH, ACTH, cortisol and prolactin during sleep in healthy volunteers. Psychoneuroendocrinology. 2004 Aug;29(7):851-60. PubMed PMID: 15177700. 16: Puechagut PB, Martini AC, Stutz G, Santillán ME, Luque EM, Fiol de Cuneo M, Ruiz RD, Vincenti LM. Reproductive performance and fertility in male and female adult mice chronically treated with hexarelin. Reprod Fertil Dev. 2012;24(3):451-60. doi: 10.1071/RD11009. PubMed PMID: 22401277. 17: Pang JJ, Xu RK, Xu XB, Cao JM, Ni C, Zhu WL, Asotra K, Chen MC, Chen C. Hexarelin protects rat cardiomyocytes from angiotensin II-induced apoptosis in vitro. Am J Physiol Heart Circ Physiol. 2004 Mar;286(3):H1063-9. PubMed PMID: 14615277. 18: Prodam F, Benso A, Gramaglia E, Lucatello B, Riganti F, van der Lely AJ, Deghenghi R, Muccioli G, Ghigo E, Broglio F. Cortistatin-8, a synthetic cortistatin-derived ghrelin receptor ligand, does not modify the endocrine responses to acylated ghrelin or hexarelin in humans. Neuropeptides. 2008 Feb;42(1):89-93. PubMed PMID: 18061663. 19: Orkin RD, New DI, Norman D, Chew SL, Clark AJ, Grossman AB, Korbonits M. Rapid desensitisation of the GH secretagogue (ghrelin) receptor to hexarelin in vitro. J Endocrinol Invest. 2003 Aug;26(8):743-7. PubMed PMID: 14669829. 20: Pettersson I, Muccioli G, Granata R, Deghenghi R, Ghigo E, Ohlsson C, Isgaard J. Natural (ghrelin) and synthetic (hexarelin) GH secretagogues stimulate H9c2 cardiomyocyte cell proliferation. J Endocrinol. 2002 Oct;175(1):201-9. PubMed PMID: 12379504.

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