Tesamorelin Technical Specification Sheet
Molecular Properties
| Parameter |
Value |
| Chemical Name |
Tesamorelin / TH9507 / Trans-3-Hexenoyl-GHRH(1-44)-NH₂ |
| Amino Acid Sequence |
Hexanoyl-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu-NH₂ |
| Molecular Formula |
C₂₂₁H₃₆₆N₇₂O₆₇S |
| Molecular Weight |
5135.89 g/mol |
| CAS Number |
218949-48-5 |
| Sequence Length |
44 amino acids + N-terminal hexenoyl modification |
| Receptor Target |
Growth hormone-releasing hormone receptor (GHRHR) |
Physical Properties
| Property |
Specification |
| Appearance |
White to off-white sterile lyophilized powder |
| Solubility |
Soluble in water or bacteriostatic water at ≥1 mg/mL; improved vs native GHRH |
| pH (1% solution) |
6.5 - 8.0 |
| Hygroscopicity |
Moderate; desiccated storage required |
| Solution Stability |
Stable at 4°C for 7-14 days; superior to unmodified GHRH |
Analytical Specifications
| Test |
Specification |
| HPLC Purity |
≥98.0% |
| Mass Spectrometry |
Confirmed [M+H]⁺ = 5135.89 ± 2.0 Da |
| Peptide Content |
≥90% (by amino acid analysis) |
| Endotoxin Level |
<1.0 EU/mg |
| Acetate Content |
≤8% |
| TFA Content |
≤0.5% |
| Water Content |
≤8% (Karl Fischer) |
Storage Parameters
| Condition |
Specification |
| Lyophilized Storage |
-20°C to -80°C, desiccated, protected from light |
| Lyophilized Shelf Life |
24-36 months when stored properly |
| Reconstituted Storage |
2-8°C for up to 14 days; -20°C for up to 3 months |
| Reconstitution Protocol |
Add 2 mL bacteriostatic water to 2 mg vial; gently swirl (do not shake vigorously) for 1-2 minutes |
| Freeze-Thaw Cycles |
Maximum 3 cycles; aliquot for single use recommended |
| Light Sensitivity |
Moderate; store in amber vials |
Research Dosing Reference
| Application |
Typical Dose Range |
Frequency |
Route |
| In Vitro Pituitary Cell Assays |
1-100 nM |
Acute stimulation (30 min to 4 hours) |
Culture media |
| Small Animal Models (Rodent) |
50-500 μg/kg |
Daily, typically evening administration |
SC injection |
| GH Secretion Studies |
100-300 μg/kg |
Once daily for 7-28 days |
SC preferred |
| Metabolic Research |
1-3 mg/kg |
Daily for 4-12 weeks |
SC injection |
Note: Dosing information is for research reference only. Tesamorelin is intended for laboratory research. Hexenoyl modification increases stability and potency vs native GHRH.
Key Research Studies
| Year |
Study Focus |
Key Findings |
| 2005 |
Hexenoyl modification and stability enhancement |
Trans-3-hexenoyl N-terminal modification increased plasma half-life 3-5 fold vs native GHRH(1-44); maintained full agonist activity at GHRHR with EC₅₀ ~0.5-2 nM for GH release |
| 2010 |
Visceral adipose tissue reduction |
Daily tesamorelin (2 mg SC) for 26 weeks reduced visceral adipose tissue by 15-18%; increased IGF-1 levels by 50-80%; improved lipid profiles without significant effects on glucose metabolism |
| 2014 |
Pharmacokinetics and GH pulsatility |
Single SC dose (2 mg) produced peak GH levels at 0.5-1 hour; GH elevation sustained 3-4 hours; maintained physiological pulsatile GH secretion pattern (unlike continuous GH administration) |
| 2018 |
Cognitive function and hippocampal effects |
Chronic tesamorelin treatment (20 weeks) improved working memory performance; increased hippocampal volume by 5-7% on MRI; enhanced functional connectivity in cognitive networks |
Mechanism of Action
| Biological Pathway |
Description |
| GHRH Receptor Activation |
Binds GHRHR on pituitary somatotrophs; Gs-coupled receptor → adenylyl cyclase → cAMP → PKA activation → Ca²⁺ influx |
| GH Secretion |
Stimulates synthesis and pulsatile release of growth hormone from anterior pituitary; maintains physiological GH patterns (peaks 0.5-2h post-dose) |
| IGF-1 Production |
GH stimulates hepatic IGF-1 synthesis; circulating IGF-1 mediates anabolic and metabolic effects; negative feedback on GH secretion |
| Metabolic Effects |
Lipolysis in adipocytes (particularly visceral fat); increased lean body mass; enhanced protein synthesis; modulation of glucose and lipid metabolism |
| Half-Life |
30-60 minutes (SC); hexenoyl modification protects from rapid enzymatic degradation (vs 6-8 min for native GHRH) |
Comparative Analysis: GHRH Analogs
| Compound |
Structure |
Half-Life |
Key Feature |
| Native GHRH(1-44) |
44 amino acids, unmodified |
6-8 minutes |
Rapid degradation; clinical use limited |
| Tesamorelin |
44 aa + N-terminal hexenoyl |
30-60 minutes |
Enhanced stability; approved for lipodystrophy |
| Sermorelin |
29 amino acids (GHRH 1-29) |
10-20 minutes |
Shorter sequence; retains full activity |
| CJC-1295 |
30 aa + DAC modification |
6-8 days |
Prolonged action; non-physiological |
Quality Control Parameters
| Test Method |
Acceptance Criteria |
| Appearance (visual) |
White to off-white cake; no discoloration |
| Hexenoyl Modification |
N-terminal trans-3-hexenoyl confirmed by MS/MS; >95% modified |
| RP-HPLC (purity) |
Main peak ≥98.0%; no single impurity >0.5% |
| ESI-MS (identity) |
[M+H]⁺ = 5135.89 ± 2.0 Da confirmed |
| Biological Activity |
≥85% potency vs reference in GH release assay |
Reported Biological Effects
| Effect Category |
Observed Changes |
Timeframe |
| GH/IGF-1 Axis |
Increased GH secretion (peak 0.5-1h); IGF-1 elevation 50-100% within 1-2 weeks |
Acute to 2 weeks |
| Body Composition |
Reduced visceral adipose tissue 10-20%; increased lean body mass 2-5% |
12-26 weeks |
| Lipid Profile |
Decreased triglycerides 15-25%; modest improvement in LDL/HDL ratio |
8-16 weeks |
| Cognitive Effects |
Improved working memory; increased hippocampal volume; enhanced executive function |
12-20 weeks |
Disclaimer: This product is intended for research use only. Not for human or veterinary diagnostic or therapeutic use. Tesamorelin is a modified GHRH analog with enhanced pharmacokinetic properties.