Sermorelin
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Research Use Only
These products are for laboratory research only and not intended for medical use. They are not FDA-approved to diagnose, treat, cure, or prevent any disease. By purchasing, you certify they will be used solely for research and not for human or animal consumption.
Research Summary
20 PubMed CitationsSermorelin (GHRH 1-29) is a synthetic 29-amino acid peptide with a molecular weight of 3,357.88 Da. It corresponds to the N-terminal segment of the endogenous 44-amino acid GHRH molecule and is considered the shortest fully functional fragment retaining full biological activity. [1] [2] Key Features: Binding Potency: Equipotent to full-length GHRH(1-40) in stimulating GH secretion Pulsatility: Stimulates natural pulsatile GH release (unlike rhGH) Feedback: Regulated by somatostatin — overdose difficult Gene Transcription: Stimulates hGH mRNA transcription, increases pituitary reserve [3] Regulatory Status: FDA: Approved 1990 (diagnostic) / 1997 (pediatric GHD) as Geref. Voluntarily discontinued 2008 — NOT for tolerability/efficacy reasons. Now available compounded. [4] WADA: Prohibited (S2 — Peptide Hormones). [5] Developer: EMD Serono, Inc. (formerly Serono Laboratories) Pharmacokinetic Highlights: Bioavailability: ~6% (SC); ~5.1% in rats Half-Life: ~11–12 min (SC/IV) Tmax: 5–20 min (SC) Clearance: 2.4–2.8 L/min Route: SC injection (primary), IV (diagnostic) Discovery and historical context. Sermorelin was developed...
Sermorelin — Research Data at a Glance
| Property | Value |
|---|---|
| Molecular Formula | C₁₄₉H₂₄₆N₄₄O₄₂S |
| Molecular Weight | 3,357.88 Da |
| CAS Number | 86168-78-7 |
| Amino Acid Sequence | YADAIFTNSYRKVLGQLSARKLLQDIMSR-NH₂ (29 aa) |
| PubMed Citations Referenced | 20 |
| Contributing Researchers | 3 |
| Storage Conditions | Lyophilized: 2–8°C refrigerated, protect from light. |
| Purity Standard | ≥99% (HPLC verified, 3rd-party COA) |
| Research Use Only | Not for human consumption. RUO only. |
Compare Sermorelin with Other Peptides
Overview
Sermorelin (GHRH 1-29) is a synthetic 29-amino acid peptide with a molecular weight of 3,357.88 Da. It corresponds to the N-terminal segment of the endogenous 44-amino acid GHRH molecule and is considered the shortest fully functional fragment retaining full biological activity. [1] [2]
Key Features:
- Binding Potency: Equipotent to full-length GHRH(1-40) in stimulating GH secretion
- Pulsatility: Stimulates natural pulsatile GH release (unlike rhGH)
- Feedback: Regulated by somatostatin — overdose difficult
- Gene Transcription: Stimulates hGH mRNA transcription, increases pituitary reserve [3]
Regulatory Status:
- FDA: Approved 1990 (diagnostic) / 1997 (pediatric GHD) as Geref. Voluntarily discontinued 2008 — NOT for tolerability/efficacy reasons. Now available compounded. [4]
- WADA: Prohibited (S2 — Peptide Hormones). [5]
Developer: EMD Serono, Inc. (formerly Serono Laboratories)
Pharmacokinetic Highlights:
- Bioavailability: ~6% (SC); ~5.1% in rats
- Half-Life: ~11–12 min (SC/IV)
- Tmax: 5–20 min (SC)
- Clearance: 2.4–2.8 L/min
- Route: SC injection (primary), IV (diagnostic)
Discovery and historical context. Sermorelin was developed in the 1980s following the structural elucidation of human GHRH by Roger Guillemin and colleagues. Subsequent fragment-truncation studies established that the N-terminal 29 amino acids contain the full receptor-binding and signal-transduction activity of the parent 44-amino-acid hormone, leading to commercial development of GRF(1-29)-NH2 as a research and diagnostic tool. [1] [2] The peptide is biologically equipotent to full-length GHRH on a molar basis but is more economical to synthesize, which is why nearly all GHRH-pathway research published after 1985 uses sermorelin rather than the native 1-44 sequence. [6]
Research framework. Sermorelin is widely used as the canonical GHRH-receptor probe in studies of pituitary somatotroph physiology, GH/IGF-1 axis aging, and pulsatile neuroendocrine secretion. Because endogenous somatostatin remains in the loop, sermorelin produces a self-limiting pulsatile GH burst rather than the sustained supraphysiologic exposure produced by exogenous recombinant human GH (rhGH) — an important distinction for research models examining GH receptor desensitization, IGF-1 feedback, and counter-regulatory hormone responses. [3] Closely related GHRH-pathway research compounds include tesamorelin (a DPP-4-resistant 44-amino-acid GHRH analog), CJC-1295 (an albumin-binding GHRH analog with extended half-life), and ipamorelin (a complementary GHS-R1a-pathway peptide). [7]
Mechanism of Action
1. Receptor Target — GHRH Receptor
Sermorelin binds specifically to the GHRH receptor (GHRHR) on somatotroph cells in the anterior pituitary gland. Despite being a 29-aa fragment, it is equipotent to full-length GHRH(1-40) in stimulating GH secretion. [1] [6]
2. Downstream Signaling Cascades
Upon binding to the GHRHR, Sermorelin activates multiple intracellular pathways:
- Gₛ/Adenylyl Cyclase → cAMP Pathway: Primary mechanism — receptor activation triggers Gₛα, stimulating adenylyl cyclase to produce cAMP as a second messenger [6]
- MAPK Pathway: GHRHR activation also stimulates the mitogen-activated protein kinase pathway [6]
- Ca²⁺ Signaling: Cascades raise intracellular calcium levels, facilitating vesicle fusion and exocytosis of growth hormone
🔑 Pulsatile GH Release: Unlike exogenous rhGH, Sermorelin stimulates the pituitary to release GH in natural bursts/pulses, mimicking neuroendocrine rhythms and avoiding tachyphylaxis. Its action is regulated by somatostatin negative feedback, making overdose difficult. [3]
The product supplied here is for research use only regardless of regulatory status of related formulations.
3. Dose-Response Characteristics
- Duration vs Peak: The duration of GH release is more dose-dependent than peak magnitude [6]
- Elderly Restoration: High-dose Sermorelin (1 mg BID) restores IGF-1 in elderly men to young adult levels [7]
- In Vitro Sensitivity: Minimal effective dose in rat pituitary cultures: 0.4 × 10⁻¹⁵ M [8]
4. Receptor Selectivity
In vitro: Does NOT stimulate LH, FSH, or Prolactin release (high somatotroph selectivity). [8]
In vivo (human): Minor acute rises in prolactin, FSH, and LH reported in children — effect not seen with GHRH(1-40) — suggesting slight differences between fragment and full-length. [9]
5. Cellular and Tissue-Level Effects
Anti-Tumor (Glioma):
- Blocks cell cycle progression in recurrent glioma cells
- Negatively regulates immune checkpoints, downregulates GHRHR/GGF
- Identified as most effective candidate from 4,865 drugs (P<0.0001) [10]
Immune Activation:
- Increases B cell number (~30%) and responsiveness to mitogens (+50%)
- Increases lymphocytes expressing IL-2 receptors (+70%)
- Enhances T cell responsiveness to phytohemagglutinin (+50%) [11]
6. Comparison to Related Compounds
| Compound | Structure | Key Difference |
|---|---|---|
| Sermorelin | 29 aa (native fragment) | Shortest functional GHRH; T½ ~11 min; equipotent to 1-40 |
| Tesamorelin | 44 aa + hexenoyl cap | DPP-4 resistant; T½ ~30 min; more potent |
| D-Ala²-GHRH(1-29) | 29 aa + D-Ala² | Lower clearance; longer T½ than native fragment |
| CJC-1295 + DAC | GHRH analog + DAC | Days-long T½ via albumin binding; continuous GH |
| Somatropin (rhGH) | Exogenous GH | Bypasses pituitary; constant levels; higher risk |
7. Pharmacokinetics
| Parameter | Value |
|---|---|
| Route | SC (experimental), IV (diagnostic) |
| Bioavailability | ~6% (SC); ~5.1% in rats |
| Half-Life (T½) | ~11–12 min (SC/IV); ~6.2 min in rats |
| Tmax | 5–20 min (SC) |
| Clearance | 2.4–2.8 L/min (adults) |
| GH Pulsatility | Preserved (natural pulses, somatostatin feedback intact) |
| Metabolism | DPP-4 proteolysis; no N-terminal modification |
Research Applications
👶 Pediatric GHD (Formerly FDA-registered)
The Geref International Study Group multicenter trial (n=110) established Sermorelin for pediatric GH deficiency. Growth velocity increased from 4.1 cm/yr to 8.0 cm/yr at 6 months, with 74% good response rate. No excessive IGF-1 generation or glucose changes. [2]
🔬 Diagnostic Evaluation
A single IV dose (1 µg/kg) is used to assess pituitary GH reserve, distinguishing hypothalamic vs pituitary causes of GHD. Fewer false positives compared to other provocative tests. [2]
🧓 Anti-Aging / Age-Related GH Decline
In healthy elderly subjects (n=19), 16-week research application produced +107% nocturnal GH (men), +1.26 kg lean mass, improved insulin sensitivity, and enhanced well-being. High-dose (1 mg BID) restored IGF-1 to young adult levels in men aged 60–78. [7] [12]
🧠 Cognitive Function & Sleep
Sermorelin facilitates slow-wave sleep, which is correlated with nocturnal GH secretion. Modulates age-related decline in the somatotropic axis. [13]
🛡️ Immunosenescence
In aging adults, Sermorelin significantly enhanced immune function: B cell +30%, T cell responsiveness +50–70%, IL-2 receptor expression +70%, transient IgG/IgM/IgA increases. [11]
💪 Body Composition / Hypogonadal Men
A retrospective study (n=14) of hypogonadal men on testosterone + Sermorelin/GHRP-2/GHRP-6 showed significant IGF-1 increases at 90, 180, and 270 days. Lean body mass and visceral fat improvements. [14]
🎯 Oncology — Glioma
Bioinformatics screening of 4,865 drugs identified Sermorelin as the most effective candidate for recurrent glioma (P<0.0001). In vitro, it inhibited U87/LN229 cell growth dose-dependently by blocking cell cycle and negatively regulating immune checkpoints. [10]
GHRH-Receptor Pulsatility and Somatostatin-Feedback Profiling
Sermorelin is used as a research tool to investigate whether stimulating endogenous, pulsatile GH secretion through the GHRH receptor preserves the natural somatostatin negative-feedback loop and yields a different IGF-1 and metabolic-substrate signature compared to continuous exogenous recombinant human GH. Comparative ultradian profiling studies in young versus elderly cohorts have catalogued amplitude, frequency, and trough patterns useful for modelling natural-pulsatility versus tonic-elevation GH biology. [7]
Comparative Research Context
Within the GHRH-axis research family, sermorelin is most directly compared with tesamorelin (full-length GHRH(1-44) with N-terminal acylation for DPP-4 resistance), CJC-1295 (long-acting GHRH analog), and the lipolytic hGH-fragment AOD-9604. These cross-comparisons inform research designs investigating whether truncated GHRH(1-29), full-length GHRH(1-44), or albumin-binding long-acting GHRH analogs produce distinct downstream IGF-1 and substrate-handling phenotypes.
Biochemical Characteristics
| Property | Value |
|---|---|
| Formula | C₁₄₉H₂₄₆N₄₄O₄₂S |
| Molecular Weight | 3,357.88 Da |
| Synonyms | Sermorelin acetate, Geref, GRF 1-29 NH₂, GHRH(1-29), Growth Hormone-Releasing Factor (1-29) amide, Somatotropin-releasing-hormone(1-29)amide |
| Cas Number | 86168-78-7 |
| Sequence | YADAIFTNSYRKVLGQLSARKLLQDIMSR-NH₂ (29 aa) |
| Pubchem Cid | 16129620 / 16132413 |
| Monoisotopic Mass | 3,355.818 Da |
| Polar Area | N/A |
| Complexity | N/A |
| X Log P | N/A |
| Heavy Atom Count | N/A |
| H Bond Donor Count | N/A |
| H Bond Acceptor Count | N/A |
| Rotatable Bond Count | N/A |
Identifiers
| Pubchem Cid | |
|---|---|
| Inchi Key | |
| Inchi | |
| Smiles Isomeric | |
| Smiles Canonical | |
| Iupac Name |
Preclinical Research Summary
Clinical Studies
🏛️ Sermorelin is the classic GHRH fragment — formerly FDA-registered, with a robust tolerability record spanning pediatric, geriatric, and diagnostic applications. Its pulsatile GH release and somatostatin regulation provide a unique tolerability profile.
| Study | Type | n= | Indication | Key Result | Outcome |
|---|---|---|---|---|---|
| Khorram 1997 (Metabolic) | RCT | 19 | Healthy Elderly | +107% nocturnal GH (men), +1.26 kg lean mass | ✅ Positive |
| Khorram 1997 (Immune) | RCT | 19 | Healthy Elderly | +30% B cells, +50% T-cell responsiveness | ✅ Positive |
| Vittone 1997 | Prospective | 11 | Elderly Men | 2x 12h GH release, improved muscle strength | ✅ Positive |
| Corpas 1992 | Dose-ranging | 19 | Young vs Elderly | High-dose restored IGF-1 to young adult levels | ✅ Positive |
| Sigalos 2017 | Retrospective | 14 | Hypogonadal Men | Significant IGF-1 increase at 90, 180, 270 days | ✅ Positive |
| Thorner 1996 (Geref ISG) | Multicenter OL | 110 | Pediatric GHD | 8.0 cm/yr (from 4.1), 74% good response | ✅ Positive |
| Diagnostic | Standard | — | Pituitary Function | 1 µg/kg IV; fewer false positives | ✅ Standard |
| Veldhuis 2008 | Physiology | 22 | GH Burst Waveform | GHRH+GHRP-2 → 54x GH mass vs saline | ✅ Positive |
Reported Tolerability Profile
Sermorelin has a well-established tolerability record from FDA-registered experimental investigation. [4]
- Common: Injection site reactions (~16%), transient facial flushing, headache, nausea, dizziness
- Immunogenicity: Up to 70% develop anti-GRF antibodies with chronic use — typically non-neutralizing, do not affect efficacy
- Rare: Dysphagia, hyperactivity, somnolence, urticaria, chest tightness
- Reproductive: Pregnancy Category C — minor fetal variations in rats/rabbits at 3–6x human dose
- Contraindications: Active malignancy, untreated hypothyroidism, hypersensitivity, pregnancy
- Key Regulatory Note: FDA confirmed Geref was NOT withdrawn for tolerability or efficacy reasons [4]
ALL ARTICLES AND PRODUCT INFORMATION PROVIDED ON THIS WEBSITE ARE FOR INFORMATIONAL AND EDUCATIONAL PURPOSES ONLY.
Authors & Attribution
✍️ Article Author
Dr. Michael O. Thorner
Michael O. Thorner, MB, BS, DSc, is Professor Emeritus at the University of Virginia. He led the Geref International Study Group multicenter trials that established Sermorelin's efficacy in pediatric GHD. A pioneer in GHRH discovery, his work spans from the original characterization of GHRH to modern growth hormone secretagogue research for aging. Michael O. Thorner is being referenced as one of the leading scientists involved in the research and development of Sermorelin. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Pure US Peptide and this doctor.
View Full Researcher Profile →🎓 Scientific Journal Author
Dr. Andrew V. Schally
Andrew V. Schally, PhD, is a Nobel Prize laureate (1977) and Distinguished Medical Research Scientist at the VA Medical Center Miami and University of Miami. He spent decades developing GHRH analogs including agonists and antagonists, with major contributions to understanding oncological applications of GHRH peptides in glioblastoma, lung, and prostate cancer via GHRH receptor downregulation. Andrew V. Schally is being referenced as one of the leading scientists involved in the research and development of Sermorelin. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Pure US Peptide and this doctor.
View Full Researcher Profile →Dr. Andrew V. Schally is being referenced as one of the leading scientists involved in the research and development of Sermorelin. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Pure US Peptide and this doctor. The purpose of citing the doctor is to acknowledge, recognize, and credit the exhaustive research and development efforts conducted by the scientists studying this peptide.
🔬 Contributing Researcher
Dr. Richard F. Walker
Richard F. Walker, PhD, is affiliated with the International Society for Applied Research in Aging (SARA) and serves as Editor-in-Chief of Clinical Interventions in Aging. He has been a significant proponent of Sermorelin for adult-onset GH insufficiency and anti-aging research compound, publishing key editorials on its physiological advantages over rhGH including preserved pulsatile GH release and neuroendocrine function. Richard F. Walker is being referenced as one of the leading scientists involved in the research and development of Sermorelin. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Pure US Peptide and this doctor.
View Full Researcher Profile →Dr. Richard F. Walker is being referenced as one of the leading scientists involved in the research and development of Sermorelin. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Pure US Peptide and this doctor. The purpose of citing the doctor is to acknowledge, recognize, and credit the exhaustive research and development efforts conducted by the scientists studying this peptide.
Referenced Citations
Chang Y, Huang R, Zhai Y, et al. A potentially effective compound for study subjects with recurrent glioma: sermorelin. Ann Transl Med, 9(5), 406, 2021.
PubMedPrakash A, Goa KL. Sermorelin: a review of its use in the diagnosis and investigation of children with idiopathic growth hormone deficiency. BioDrugs, 12(2), 139-157, 1999.
PubMedWalker RF. Sermorelin: a better approach to management of adult-onset growth hormone insufficiency? Clin Interv Aging, 1(4), 307-308, 2006.
PubMedFood and Drug Administration. Determination That GEREF (Sermorelin Acetate) Injection Was Not Withdrawn From Sale for Reasons of tolerability or Effectiveness. Fed Register, 78(42), 14095-14096, 2013.
SourceSinha DK, Balasubramanian A, Tatem AJ, et al. Beyond the androgen receptor: the role of growth hormone secretagogues in the modern management of body composition in hypogonadal males. Transl Androl Urol, 9(Suppl 2), S149-S159, 2020.
PubMedGrossman AB, Savage MO, Lytras N, Besser GM. Responses to analogues of growth hormone releasing hormone in normals and in GH-deficient children and young adults. Clin Endocrinol (Oxf), 21(3), 321-330, 1984.
PubMedCorpas E, Harman SM, Piñeyro MA, et al. Growth hormone (GH)-releasing hormone-(1-29) twice daily reverses the decreased GH and insulinlike growth factor-I levels in old men. J Clin Endocrinol Metab, 75(2), 530-535, 1992.
PubMedHeiman ML, Nekola MV, Murphy WA, Lance VA, Coy DH. An extremely sensitive in vitro model for elucidating structure-activity relationships of growth hormone-releasing factor analogs. Endocrinology, 116(1), 410-415, 1985.
PubMedGelander L, Lindstedt G, Selstam G, et al. Effects of acute IV injection of two growth hormone-releasing hormones on serum GH and other pituitary hormones in short children. Horm Res, 31(5-6), 213-220, 1989.
PubMedKhorram O, Laughlin GA, Yen SS. Endocrine and metabolic effects of long-term administration of [Nle27]GHRH-(1-29)-NH2 in age-advanced men and women. J Clin Endocrinol Metab, 82(5), 1472-1479, 1997.
PubMedKhorram O, Yeung M, Vu L, Yen SS. Effects of [norleucine27]growth hormone-releasing hormone (GHRH) (1-29)-NH2 administration on the immune system of aging men and women. J Clin Endocrinol Metab, 82(11), 3590-3596, 1997.
PubMedVittone J, Blackman MR, Busby-Whitehead J, et al. Effects of single nightly injections of GHRH 1-29 in healthy elderly men. Metabolism, 46(1), 89-96, 1997.
PubMedVitiello MV, Schwartz RS, Moe KE, Mazzoni G, Merriam GR. Treating age-related changes in somatotrophic hormones, sleep, and cognition. Dialogues Clin Neurosci, 3(3), 229-236, 2001.
PubMedSigalos JT, Pastuszak AW, Allison A, et al. Growth Hormone Secretagogue research application in Hypogonadal Men Raises Serum IGF-1 Levels. Am J Mens Health, 11(6), 1752-1757, 2017.
PubMedSchally AV, Wang H, He J, et al. Agonists of growth hormone-releasing hormone (GHRH) inhibit human experimental cancers in vivo by down-regulating receptors for GHRH. PNAS, 115(47), 12028-12033, 2018.
PubMedJaszberenyi M, Rick FG, Popovics P, et al. Potentiation of cytotoxic chemotherapy by growth hormone-releasing hormone agonists. PNAS, 111(2), 781-786, 2014.
PubMedSoule SG, King JA, Millar RP. Incorporation of D-Ala2 in GHRH-(1-29)-NH2 increases half-life and decreases metabolic clearance in normal men. J Clin Endocrinol Metab, 79(4), 1208-1211, 1994.
PubMedMerriam GR, Buchner DM, Prinz PN, Schwartz RS, Vitiello MV. Potential applications of GH secretagogs in the evaluation and investigation of the age-related decline in GH secretion. Endocrine, 7(1), 49-52, 1997.
PubMedWalker RF, Yang SW, Bercu BB. Robust Growth Hormone (GH) secretion in aged female rats co-administered GH-releasing hexapeptide (GHRP-6) and GH-releasing hormone (GHRH). Life Sci, 49(20), 1499-1504, 1991.
PubMedRafferty B, Coy DH, Poole S. Pharmacokinetic evaluation of superactive analogues of growth hormone-releasing factor (1-29)-amide. Peptides, 9(1), 207-209, 1988.
PubMedRUO Disclaimer
For Research Use Only (RUO). Not intended for human consumption, clinical use, or as a drug, food, cosmetic, or medical device. This product has not been evaluated by the FDA and is supplied solely for in-vitro laboratory research by qualified professionals.
Certificate of Analysis
Each lot is independently tested by accredited third-party laboratories (ISO 17025) at 99%+ purity.
Latest Lab Report
Storage & Handling
Summary
Lyophilized: 2–8°C refrigerated, protect from light. Available in 0.5–15 mg vials (compounded). Reconstituted: 14–30 days refrigerated.
❄️ Lyophilized Powder Storage
Store unreconstituted vials refrigerated at 2°C to 8°C (36–46°F). Protect from light. The peptide is supplied as a sterile, non-pyrogenic, lyophilized powder with mannitol as a stabilizing agent.
💧 Reconstitution
Reconstitute with Bacteriostatic Water for Injection or Sodium Chloride Injection, USP. Swirl gently — do NOT shake. Vigorous shaking can denature the peptide structure. Solution should be clear; discard if cloudy.
⏰ Reconstituted Stability
- Refrigerated (2–8°C): 14–30 days (varies by formulation/pharmacy)
- Do not freeze
- Check specific pharmacy guidelines for your formulation
📊 Available Vial Sizes
- 0.5 mg, 3.0 mg, 6 mg, 9 mg, 15 mg (compounded formulations)
- Alternative forms: Orally disintegrating tablets (ODTs), nasal sprays (compounded)
🔬 Quality Verification
Purity verified via HPLC and Mass Spectrometry (≥98% peptide purity). Compounded formulations undergo sterility testing (USP <71>). This product is for research use only (RUO).
“Clinical Studies 🏛️ Sermorelin is the classic GHRH fragment — formerly FDA-registered, with a robust tolerability record spanning pediatric, geriatric, and diagnostic applications.”
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