Hexarelin

Key Benefits#

• Strongest GH pulse per mcg among GHRPs
• Unique direct cardioprotective effects via CD36
• Increased IGF-1 and muscle anabolism
• Accelerated recovery from training
• Bone density support
• Anti-aging via GH axis
• Potential cardiac rehabilitation benefits

Mechanism of Action#

Hexarelin activates ghrelin receptors (GHSR-1a) with greater potency than GHRP-2 or GHRP-6, producing the largest acute GH pulses among synthetic GHRPs. Uniquely, it also binds CD36 receptors on cardiac cells, providing cardioprotective effects independent of GH secretion. These include protection against ischemia-reperfusion injury and cardiac hypertrophy. However, it undergoes more pronounced receptor desensitization with continuous use compared to other GHRPs.

Dosing Protocols#

Side Effects#

• Water retention
• Elevated cortisol
• Elevated prolactin (more pronounced than other GHRPs)
• Receptor desensitization with continuous use
• Increased appetite

Contraindications#

Active cancer or history of cancer. Pregnancy or breastfeeding. Hyperprolactinemia.

Storage#

Lyophilized powder: store at −20°C. Reconstituted: refrigerate at 2–8°C, use within 30 days.

Featured In Stacks#

1. 1.
   Identification of alexamorelin consumption biomarkers using human hepatocyte incubations and high-resolution mass spectrometry

   Pobee E, Daziani G, Gameli PS, Basile G, Carlier J, Tini A · Journal of analytical toxicology · 2025PubMed Verified

2. 2.
   Pharmacological targeting of the hyper-inflammatory response to SARS-CoV-2-infected K18-hACE2 mice using a cluster of differentiation 36 receptor modulator

   Gauvin J, Huynh DN, Dubuc I, Lê C, Tugores R, Flamand N et al. · Frontiers in pharmacology · 2024PubMed Verified

3. 3.
   Revealing the interaction between peptide drugs and permeation enhancers in the presence of intestinal bile salts

   Hossain S, Kneiszl R, Larsson P · Nanoscale · 2023PubMed Verified

4. 4.
   Hexarelin alleviates apoptosis on ischemic acute kidney injury via MDM2/p53 pathway

   Guan C, Li C, Shen X, Yang C, Liu Z, Zhang N et al. · European journal of medical research · 2023PubMed Verified

5. 5.
   Protective Effects of Hexarelin and JMV2894 in a Human Neuroblastoma Cell Line Expressing the SOD1-G93A Mutated Protein

   Meanti R, Licata M, Rizzi L, Bresciani E, Molteni L, Coco S et al. · International journal of molecular sciences · 2023PubMed Verified

6. 6.
   Using Synchrotron Radiation Imaging Techniques to Elucidate the Actions of Hexarelin in the Heart of Small Animal Models

   Waddingham MT, Tsuchimochi H, Sonobe T, Asano R, Jin H, Ow CPC et al. · Frontiers in physiology · 2021PubMed Verified

7. 7.
   Hexarelin modulates lung mechanics, inflammation, and fibrosis in acute lung injury

   Zambelli V, Rizzi L, Delvecchio P, Bresciani E, Rezoagli E, Molteni L et al. · Drug target insights · 2021PubMed Verified

8. 8.
   Hexarelin attenuates abdominal aortic aneurysm formation by inhibiting SMC phenotype switch and inflammasome activation

   Jiang B, Wang M, Li X, Ren P, Li G, Wang Y et al. · Microvascular research · 2022PubMed Verified

9. 9.
   Effect of paracellular permeation enhancers on intestinal permeability of two peptide drugs, enalaprilat and hexarelin, in rats

   Dahlgren D, Olander T, Sjöblom M, Hedeland M, Lennernäs H · Acta pharmaceutica Sinica. B · 2021PubMed Verified

10. 10.
    Hexarelin Modulation of MAPK and PI3K/Akt Pathways in Neuro-2A Cells Inhibits Hydrogen Peroxide-Induced Apoptotic Toxicity

    Meanti R, Rizzi L, Bresciani E, Molteni L, Locatelli V, Coco S et al. · Pharmaceuticals (Basel, Switzerland) · 2021PubMed Verified

11. 11.
    Stimulation of endogenous pulsatile growth hormone secretion by activation of growth hormone secretagogue receptor reduces the fat accumulation and improves the insulin sensitivity in obese mice

    Huang Z, Lu X, Huang L, Zhang C, Veldhuis JD, Cowley MA et al. · FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2021PubMed Verified

12. 12.
    Ghrelin receptor agonist hexarelin attenuates antinociceptive tolerance to morphine in rats

    Baser T, Ozdemir E, Filiz AK, Taskiran AS, Gursoy S · Canadian journal of physiology and pharmacology · 2021PubMed Verified

13. 13.
    Hexarelin targets neuroinflammatory pathways to preserve cardiac morphology and function in a mouse model of myocardial ischemia-reperfusion

    McDonald H, Peart J, Kurniawan ND, Galloway G, Royce SG, Samuel CS et al. · Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2020PubMed Verified

14. 14.
    The In Vivo Effect of Transcellular Permeation Enhancers on the Intestinal Permeability of Two Peptide Drugs Enalaprilat and Hexarelin

    Dahlgren D, Sjöblom M, Hedeland M, Lennernäs H · Pharmaceutics · 2020PubMed Verified

15. 15.
    Hexarelin protects cardiac H9C2 cells from angiotensin II-induced hypertrophy via the regulation of autophagy

    Agbo E, Li MX, Wang YQ, Saahene RO, Massaro J, Tian GZ · Die Pharmazie · 2019PubMed Verified

16. 16.
    Hexarelin attenuates atherosclerosis via inhibiting LOX-1-NF-κB signaling pathway-mediated macrophage ox-LDL uptake in ApoE(-/-) mice

    Cheng XL, Ding F, Wang DP, Zhou L, Cao JM · Peptides · 2019PubMed Verified

17. 17.
    Modulation of PTEN by hexarelin attenuates coronary artery ligation-induced heart failure in rats

    Agbo E, Liu D, Li M, Saahene RO, Chen L, Zhao L et al. · Turkish journal of medical sciences · 2019PubMed Verified

18. 18.
    Characterization of a third ghrelin receptor, GHS-R3a, in channel catfish reveals novel expression patterns and a high affinity for homologous ligand

    Small BC, Quiniou SMA, Kaiya H, Bledsoe JW, Musungu B · Comparative biochemistry and physiology. Part A, Molecular & integrative physiology · 2019PubMed Verified

19. 19.
    Zebrafish (Danio rerio) water tank model for the investigation of drug metabolism: Progress, outlook, and challenges

    Sardela VF, Anselmo CS, Nunes IKDC, Carneiro GRA, Dos Santos GRC, de Carvalho AR et al. · Drug testing and analysis · 2018PubMed Verified

20. 20.
    Enhanced Pulsatile Growth Hormone Secretion and Altered Metabolic Hormones by in Vivo Hexarelin Treatment in Streptozotocin-Induced Diabetic Rats

    Zhang X, Yang JK, Chen C · International journal of molecular sciences · 2018PubMed Verified

21. 21.
    The CD36-PPARγ Pathway in Metabolic Disorders

    Maréchal L, Laviolette M, Rodrigue-Way A, Sow B, Brochu M, Caron V et al. · International journal of molecular sciences · 2018ReviewPubMed Verified

22. 22.
    Hexarelin treatment preserves myocardial function and reduces cardiac fibrosis in a mouse model of acute myocardial infarction

    McDonald H, Peart J, Kurniawan N, Galloway G, Royce S, Samuel CS et al. · Physiological reports · 2018PubMed Verified

23. 23.
    Improvement of cardiomyocyte function by in vivo hexarelin treatment in streptozotocin-induced diabetic rats

    Zhang X, Qu L, Chen L, Chen C · Physiological reports · 2018PubMed Verified

24. 24.
    Growth hormone secretagogues hexarelin and JMV2894 protect skeletal muscle from mitochondrial damages in a rat model of cisplatin-induced cachexia

    Sirago G, Conte E, Fracasso F, Cormio A, Fehrentz JA, Martinez J et al. · Scientific reports · 2017PubMed Verified

25. 25.
    Hexarelin, a Growth Hormone Secretagogue, Improves Lipid Metabolic Aberrations in Nonobese Insulin-Resistant Male MKR Mice

    Mosa R, Huang L, Wu Y, Fung C, Mallawakankanamalage O, LeRoith D et al. · Endocrinology · 2017PubMed Verified

26. 26.
    The Safety and Efficacy of Growth Hormone Secretagogues

    Sigalos JT, Pastuszak AW · Sexual medicine reviews · 2018ReviewPubMed Verified

27. 27.
    The Growth Hormone Secretagogue Hexarelin Protects Rat Cardiomyocytes From in vivo Ischemia/Reperfusion Injury Through Interleukin-1 Signaling Pathway

    Huang J, Li Y, Zhang J, Liu Y, Lu Q · International heart journal · 2017PubMed Verified

28. 28.
    Growth hormone secretagogues prevent dysregulation of skeletal muscle calcium homeostasis in a rat model of cisplatin-induced cachexia

    Conte E, Camerino GM, Mele A, De Bellis M, Pierno S, Rana F et al. · Journal of cachexia, sarcopenia and muscle · 2017PubMed Verified

29. 29.
    JMV2894, a novel growth hormone secretagogue, accelerates body mass recovery in an experimental model of cachexia

    Bresciani E, Rizzi L, Molteni L, Ravelli M, Liantonio A, Ben Haj Salah K et al. · Endocrine · 2017PubMed Verified

30. 30.
    Enhanced responsiveness of Ghsr Q343X rats to ghrelin results in enhanced adiposity without increased appetite

    Chebani Y, Marion C, Zizzari P, Chettab K, Pastor M, Korostelev M et al. · Science signaling · 2016PubMed Verified

31. 31.
    Hexarelin Protects Rodent Pancreatic Β-Cells Function from Cytotoxic Effects of Streptozotocin Involving Mitochondrial Signalling Pathways In Vivo and In Vitro

    Zhao Y, Zhang X, Chen J, Lin C, Shao R, Yan C et al. · PloS one · 2016PubMed Verified

32. 32.
    Structure-activity relationship for peptídic growth hormone secretagogues

    Ferro P, Krotov G, Zvereva I, Rodchenkov G, Segura J · Drug testing and analysis · 2017PubMed Verified

33. 33.
    Simplifying and expanding the screening for peptides <2 kDa by direct urine injection, liquid chromatography, and ion mobility mass spectrometry

    Thomas A, Görgens C, Guddat S, Thieme D, Dellanna F, Schänzer W et al. · Journal of separation science · 2016PubMed Verified

34. 34.
    Determination of growth hormone releasing peptides metabolites in human urine after nasal administration of GHRP-1, GHRP-2, GHRP-6, Hexarelin, and Ipamorelin

    Semenistaya E, Zvereva I, Thomas A, Thevis M, Krotov G, Rodchenkov G · Drug testing and analysis · 2015PubMed Verified

35. 35.
    Detection of GHRP-2 and GHRP-6 in urine samples from athletes

    Cox HD, Hughes CM, Eichner D · Drug testing and analysis · 2015PubMed Verified

36. 36.
    Implications of ghrelin and hexarelin in diabetes and diabetes-associated heart diseases

    Mosa RM, Zhang Z, Shao R, Deng C, Chen J, Chen C · Endocrine · 2015ReviewPubMed Verified

37. 37.
    In vitro models for metabolic studies of small peptide hormones in sport drug testing

    Esposito S, Deventer K, Geldof L, Van Eenoo P · Journal of peptide science : an official publication of the European Peptide Society · 2015PubMed Verified

38. 38.
    The cardiovascular action of hexarelin

    Mao Y, Tokudome T, Kishimoto I · Journal of geriatric cardiology : JGC · 2014ReviewPubMed Verified

39. 39.
    Identification, tissue distribution and functional characterization of the ghrelin receptor in West African lungfish, Protopterus annectens

    Kaiya H, Konno N, Kangawa K, Uchiyama M, Miyazato M · General and comparative endocrinology · 2014PubMed Verified

40. 40.
    We are ageing

    Kolovou GD, Kolovou V, Mavrogeni S · BioMed research international · 2014ReviewPubMed Verified

41. 41.
    One dose of oral hexarelin protects chronic cardiac function after myocardial infarction

    Mao Y, Tokudome T, Kishimoto I, Otani K, Miyazato M, Kangawa K · Peptides · 2014PubMed Verified

42. 42.
    A high-throughput LC-MS/MS screen for GHRP in equine and human urine, featuring peptide derivatization for improved chromatography

    Timms M, Hall N, Levina V, Vine J, Steel R · Drug testing and analysis · 2014PubMed Verified

43. 43.
    Scavenger receptor CD36 mediates inhibition of cholesterol synthesis via activation of the PPARγ/PGC-1α pathway and Insig1/2 expression in hepatocytes

    Rodrigue-Way A, Caron V, Bilodeau S, Keil S, Hassan M, Lévy E et al. · FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2014PubMed Verified

44. 44.
    Hexarelin treatment in male ghrelin knockout mice after myocardial infarction

    Mao Y, Tokudome T, Kishimoto I, Otani K, Hosoda H, Nagai C et al. · Endocrinology · 2013PubMed Verified

45. 45.
    Growth hormone secretagogues exert differential effects on skeletal muscle calcium homeostasis in male rats depending on the peptidyl/nonpeptidyl structure

    Liantonio A, Gramegna G, Carbonara G, Sblendorio VT, Pierno S, Fraysse B et al. · Endocrinology · 2013PubMed Verified

46. 46.
    Doping control analysis of seven bioactive peptides in horse plasma by liquid chromatography-mass spectrometry

    Kwok WH, Ho EN, Lau MY, Leung GN, Wong AS, Wan TS · Analytical and bioanalytical chemistry · 2013PubMed Verified

47. 47.
    FAT/CD36 regulates PEPCK expression in adipose tissue

    Wan Z, Matravadia S, Holloway GP, Wright DC · American journal of physiology. Cell physiology · 2013PubMed Verified

48. 48.
    Metabolism of growth hormone releasing peptides

    Thomas A, Delahaut P, Krug O, Schänzer W, Thevis M · Analytical chemistry · 2012PubMed Verified

49. 49.
    Growth hormone secretagogues preserve the electrophysiological properties of mouse cardiomyocytes isolated from in vitro ischemia/reperfusion heart

    Ma Y, Zhang L, Launikonis BS, Chen C · Endocrinology · 2012PubMed Verified

50. 50.
    Determination of prohibited, small peptides in urine for sports drug testing by means of nano-liquid chromatography/benchtop quadrupole orbitrap tandem-mass spectrometry

    Thomas A, Walpurgis K, Krug O, Schänzer W, Thevis M · Journal of chromatography. A · 2012PubMed Verified