Examorelin | Hexarelin |CAS#140703-51-1 | growth hormone-releasing factor agonist

Examorelin
featured

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

MedKoo CAT#: 530032

CAS#: 140703-51-1

Description: Examorelin, also known as Hexarelin, is a growth hormone-releasing factor (GHRF) agonist potentially for the treatment of cardiac diseases.

Chemical Structure

Examorelin

CAS# 140703-51-1

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 530032
Name: Examorelin
CAS#: 140703-51-1
Chemical Formula: C47H58N12O6
Exact Mass: 886.46
Molecular Weight: 887.060
Elemental Analysis: C, 63.64; H, 6.59; N, 18.95; O, 10.82

Price and Availability

Size	Price	Availability	Quantity
50mg	USD 1650	2 weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Hexarelin; EP-23905; MF-6003; EP23905; MF6003; EP 23905; MF 6003

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/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. 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

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.

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.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1

Volume 1

Concentration 2

Volume 2

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.

Your view history

Examorelin featured