
Front label
Growth & Peptide Secretagogues | 99.55% purity
TESAMORELIN/IPAMORELIN BLEND 11MG
- TH9507
- Egrifta
- Egrifta SV
- Egrifta WR
- Tesamorelin acetate
Tesamorelin (also known as TH9507, trade names Egrifta SV and Egrifta WR ) is a synthetic 44-amino acid growth hormone-releasing hormone (GHRH) analog developed by Theratechnologies Inc.
$120
Lot
Tl26C665
Purity (HPLC-UV/VIS)
99.55%
Lab
Vanguard Laboratory
Issued by Vanguard Laboratory, A2LA #6377.01.01. Testing was commissioned by our fulfilment partner on the material we ship; the certificate names that party, not 3rd Rock Compounds.
Quantity
TESAMORELIN/IPAMORELIN BLEND 11MG
1 vial · $120
- Third-party HPLC tested
- Lot-matched certificate
- Same-day fulfilment before 2pm
- Shipping 2–4 business days
Identifiers
- CAS number
- 218949-48-5 (free base); 901758-09-6 (acetate)
- Molecular formula
- C₂₂₁H₃₆₆N₇₂O₆₇S
- Molecular weight
- 5135.9 Da
- PubChem CID
- 16137828
- Sequence
- hexenoyl-YADAIFTNSYRKVLGQLSARKLLQDIMSRQQGESNQERGARARL-NH₂ (44 aa)
Scope of the summary below: the published literature we cite covers Tesamorelin individually. This SKU is a blend with Ipamorelin; the summary below covers one component.
Mechanism of Action
Tesamorelin acts as a specific agonist for the GHRH receptor (GHRHr), a seven-transmembrane G protein-coupled receptor (GPCR) located on somatotroph cells in the anterior pituitary gland. Binding potency is comparable to endogenous GHRH. [7]
2. DPP-4 Resistance
The trans-3-hexenoic acid modification at the N-terminal Tyr1 acts as a chemical shield against DPP-4 cleavage. Native GHRH is rapidly degraded (T½ ~5 min); Tesamorelin's modification extends stability to ~26–38 min. [3]
3. Downstream Signaling Cascade
Gₛ → Adenylyl Cyclase → cAMP → PKA → Ca²⁺ Influx → GH Exocytosis:
- Receptor activation triggers the Gₛα subunit
- Gₛα stimulates adenylyl cyclase, converting ATP to cAMP
- Elevated cAMP activates Protein Kinase A (PKA)
- PKA opens voltage-gated Ca²⁺ channels → calcium influx
- Ca²⁺ triggers exocytosis of pre-stored GH vesicles
- Simultaneously, cAMP promotes GH gene transcription (new GH synthesis) [7]
🔑 Pulsatility Preserved: Unlike exogenous rhGH (which creates constant supraphysiological levels), Tesamorelin stimulates natural pulsatile GH release. The IGF-1 negative feedback loop remains intact, preventing runaway GH production. [8]
The product supplied here is for research use only regardless of regulatory status of related formulations.
4. Selectivity
Tesamorelin is highly selective for the GHRH receptor. It does not significantly alter TSH, LH, ACTH, or Prolactin levels. Unlike GHRPs (e.g., Ipamorelin), it does not bind the ghrelin receptor. [9]
5. Cellular and Tissue-Level Effects
Adipose Tissue:
- Selectively reduces visceral adipose tissue (VAT) by ~15–18%, minimal effect on subcutaneous fat [10]
- Activates hormone-sensitive lipase (HSL), inhibits lipoprotein lipase (LPL)
- Visceral fat cells have higher GH receptor density, explaining selectivity
Hepatic (Liver):
- Reduces hepatic fat (~37% relative reduction) [11]
- Reduces de novo lipogenesis, enhances fatty acid oxidation
- Prevents progression of liver fibrosis (10.5% vs 37.5% progression, P=0.04) [11]
Musculoskeletal:
- Promotes protein synthesis, increases trunk lean mass and muscle area [12]
- Improves muscle density (myosteatosis reduction)
Nervous System:
- Improves executive function and verbal memory in MCI/aging [13]
- Increases GABA levels, modulates amyloid-beta pathways
6. Comparison with Related Molecules
| Compound | Structure | Key Difference |
|---|---|---|
| Endogenous GHRH | Native 44 aa | Rapidly degraded by DPP-4 (T½ ~5 min) |
| Tesamorelin | 44 aa + hexenoyl cap | DPP-4 resistant (T½ ~30 min); pulsatile GH |
| Sermorelin | 29 aa fragment | Shorter T½ (~5–10 min); less potent |
| CJC-1295 + DAC | GHRH analog + DAC | Days-long T½; continuous “GH bleed” (not pulsatile) |
| Somatropin (rhGH) | Exogenous GH | Bypasses pituitary; suppresses natural production |
7. Pharmacokinetics
| Parameter | Value |
|---|---|
| Route | Subcutaneous (abdomen) |
| Bioavailability | <4% (SC) |
| Half-Life (T½) | ~26–38 min (SC, 2 mg); ~11 min (1.28 mg WR) |
| Standard Dose | 2 mg SC daily (SV); 1.28 mg SC daily (WR) |
| GH Pulsatility | Preserved (natural pulses, IGF-1 feedback intact) |
| Metabolism | Proteolytic cleavage; no formal human metabolism studies |
| Animal T½ | 21–45 min (dogs) |
Preclinical Research Findings
The primary clinical application. Two pivotal Phase 3 trials (n=816) demonstrated 14–18% VAT reduction with 2 mg SC daily, with improvements in triglycerides (-12.3%), body image, and waist circumference. Reductions were maintained over 52 weeks but reversed upon discontinuation. [4] [10]
🫁 NAFLD / NASH
A 12-month RCT (n=61) in HIV-infected study subjects showed 37% hepatic fat reduction, with 35% achieving normal hepatic fat fraction (<5%). Critically, Tesamorelin prevented progression of liver fibrosis (10.5% vs 37.5% in placebo, P=0.04). [11]
🧠 Cognitive Function / MCI
In a blinded RCT (n=152) of healthy older adults and MCI study subjects, 1 mg daily for 20 weeks improved executive function (P=0.005) and global cognition (P=0.03), with IGF-1 increasing +117%. Mechanisms involve increased GABA and amyloid-beta modulation. [13]
🦴 Peripheral Nerve Regeneration
Preclinical GH models showed enhanced median nerve regeneration (axon density P<0.005, myelin thickness P<0.0001) and improved muscle re-innervation (38% vs 27.9%, P<0.02). Tesamorelin is identified as the optimal agent for human translation. [14]
❤️ Cardiovascular Risk Reduction
Reduces triglycerides and improves carotid intima-media thickness (cIMT). VAT reduction is theorized to lower atherosclerotic cardiovascular disease risk. Long-term cardiovascular outcomes remain under study. [15]
💪 Sarcopenia / Muscle Quality
Increases skeletal muscle density and area (particularly trunk region), independent of changes in muscle mass quantity. Replaces hypertrophic lipid-engorged fat cells with healthy tissue. [12]
🍬 Metabolic Syndrome / Type 2 Diabetes
A tolerability study in T2D study subjects (n=53) demonstrated neutral glucose effects — no significant changes in fasting glucose, HbA1c, or insulin response vs placebo. However, Phase 3 HIV data showed increased HbA1c risk (HR 3.3 vs placebo), warranting monitoring. [16]
GHRH-Receptor Pulsatility Profiling
Tesamorelin is used as a research tool to investigate whether stimulating endogenous, pulsatile GH secretion through the GHRH-receptor produces a different downstream IGF-1 and metabolic-substrate signature compared with continuous exogenous recombinant human GH. Pharmacokinetic-pharmacodynamic studies in healthy volunteer cohorts have catalogued amplitude, frequency, and trough patterns that inform research models of natural-pulsatility versus tonic-elevation GH biology. [7]
Comparative Research Context
Within the GHRH-axis research family, tesamorelin is most directly compared with sermorelin (truncated GHRH(1-29)), CJC-1295 (long-acting GHRH analog), and the lipolytic hGH-fragment AOD-9604. These cross-comparisons help research teams dissect GHRH-receptor-mediated visceral-adiposity effects from direct hGH-receptor or beta-3-adrenergic-driven adipocyte responses.
Safety Profile
Findings summarised above derive from in-vitro and animal studies. No safety profile for human use is established or implied, and none is offered here.
Handle as a laboratory reagent: avoid inhalation and contact, reconstitute under aseptic conditions, and observe the storage conditions below.
For research use only. Not for human consumption.
Shipping and Storage
- Supplied as lyophilised powder in a sealed vial.
- Store at 2–8°C (36–46°F). Protect from light.
- Same-day fulfilment on orders before 2pm; shipping 2–4 business days.
- For research use only. Not for human consumption.
References
- [1]Falutz J, Allas S, Kotler D, et al. A placebo-controlled, dose-ranging study of a growth hormone releasing factor in HIV-infected study subjects with abdominal fat accumulation. AIDS, 19(12), 1279-87, 2005. PubMed →
- [2]Ferdinandi ES, Brazeau P, High K, et al. Non-clinical pharmacology and tolerability evaluation of TH9507, a human growth hormone-releasing factor analogue. Basic Clin Pharmacol Toxicol, 100(1), 49-58, 2007. PubMed →
- [3]Falutz J, Allas S, Blot K, et al. Metabolic effects of a growth hormone-releasing factor in study subjects with HIV. N Engl J Med, 357(23), 2359-70, 2007. PubMed →
- [4]Falutz J, Mamputu JC, Potvin D, et al. Effects of tesamorelin (TH9507) in HIV-infected study subjects with excess abdominal fat: pooled analysis of two Phase 3 trials. J Clin Endocrinol Metab, 95(9), 4291-304, 2010.
- [5]Wang Y, Tomlinson B. Tesamorelin, a human growth hormone releasing factor analogue. Expert Opin Investig Drugs, 18(3), 303-10, 2009. PubMed →
- [6]Grunfeld C, Dritselis A, Kirkpatrick P. Tesamorelin. Nat Rev compound Discov, 10(2), 95-6, 2011. PubMed →
- [7]Stanley TL, Chen CY, Branch KL, Makimura H, Grinspoon SK. Effects of a growth hormone-releasing hormone analog on endogenous GH pulsatility and insulin sensitivity in healthy men. J Clin Endocrinol Metab, 96(1), 150-8, 2011. PubMed →
- [8]Dhillon S. Tesamorelin: a review of its use in the management of HIV-associated lipodystrophy. Drugs, 71(8), 1071-91, 2011.
- [9]Spooner LM, Olin JL. Tesamorelin: a growth hormone-releasing factor analogue for HIV-associated lipodystrophy. Ann Pharmacother, 46(2), 240-7, 2012. PubMed →
- [10]Stanley TL, Falutz J, Marsolais C, et al. Reduction in visceral adiposity is associated with an improved metabolic profile in HIV-infected study subjects receiving tesamorelin. Clin Infect Dis, 54(11), 1642-51, 2012. PubMed →
- [11]Stanley TL, Fourman LT, Feldpausch MN, et al. Effects of tesamorelin on non-alcoholic fatty liver disease in HIV: a randomised, double-blind, multicentre trial. Lancet HIV, 6(12), e821-e830, 2019. PubMed →
- [12]Adrian S, Scherzinger A, Sanyal A, et al. The Growth Hormone Releasing Hormone Analogue, Tesamorelin, Decreases Muscle Fat and Increases Muscle Area in Adults with HIV. J Frailty Aging, 8(3), 154-159, 2019.
- [13]Baker LD, Barsness SM, Borson S, et al. Effects of Growth Hormone-Releasing Hormone on Cognitive Function in Adults With Mild Cognitive Impairment and Healthy Older Adults. Arch Neurol, 69(11), 1420-9, 2012. PubMed →
- [14]Lopez J, Quan A, Budihardjo J, et al. Growth Hormone Improves Nerve Regeneration, Muscle Re-innervation, and Functional Outcomes After Chronic Denervation Injury. Sci Rep, 9(1), 3117, 2019.
- [15]Grinspoon SK, Fourman L, Stanley T, et al. Impact of Tesamorelin on Cardiovascular Disease Risk Prediction Scores: Subanalysis. Open Forum Infect Dis, 12(Suppl 1), 2025.
- [16]Clemmons DR, Miller S, Mamputu JC. tolerability and metabolic effects of tesamorelin in study subjects with type 2 diabetes: A randomized, placebo-controlled trial. PLoS One, 12(6), e0179538, 2017. PubMed →
- [17]Makimura H, Feldpausch MN, Rope AM, et al. Metabolic effects of a growth hormone-releasing factor in obese subjects with reduced growth hormone secretion. J Clin Endocrinol Metab, 97(12), 4769-79, 2012. PubMed →
- [18]Fourman LT, Czerwonka N, Feldpausch MN, et al. Visceral fat reduction with tesamorelin is associated with improved liver enzymes in HIV. AIDS, 31(16), 2253-9, 2017. PubMed →
- [19]Mangili A, Falutz J, Mamputu JC, et al. Predictors of research application response to tesamorelin in HIV-infected study subjects with excess abdominal fat. PLoS One, 10(10), e0140358, 2015.
- [20]Lake JE, La K, Erlandson KM, et al. Tesamorelin Improves Fat Quality Independent of Changes in Fat Quantity. AIDS, 35(9), 1395-1402, 2021. PubMed →
- [21]Makimura H, Murphy CA, Feldpausch MN, Grinspoon SK. The Effects of Tesamorelin on Phosphocreatine Recovery in Obese Subjects With Reduced GH. J Clin Endocrinol Metab, 99(1), 338-343, 2014.
- [22]Stanley TL, Feldpausch MN, Oh J, et al. Effect of tesamorelin on visceral fat and liver fat in HIV-infected study subjects: a randomized clinical trial. JAMA, 312(4), 380-9, 2014. PubMed →
- [23]Ellis RJ, Vaida F, Hu K, et al. Effects of Tesamorelin on Neurocognitive Impairment in Persons With HIV and Abdominal Obesity. J Infect Dis, 231(5), 1230-1238, 2025.
- [24]Falutz J, Potvin D, Mamputu JC, et al. Effects of tesamorelin in HIV-infected study subjects with abdominal fat accumulation: a randomized placebo-controlled trial with safety extension. J Acquir Immune Defic Syndr, 53(3), 311-22, 2010. PubMed →
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