Tesamorelin + Ipamorelin
Tesamorelin + Ipamorelin — reagent for research use (RUO).
Technical data
- INN name
- Tesamorelin + Ipamorelin
Sizes and prices: 17 mg $2,970 MXN ($175 MXN per mg) (sold out).
Buy Tesamorelin + Ipamorelin in Mexico: order online with nationwide shipping in 1-4 business days depending on zone and tracking number. Prices in Mexican pesos. Material for research use only.
Tesamorelin + Ipamorelin is known internationally as Tesamorelin + Ipamorelin (English INN name). Buy Tesamorelin + Ipamorelin in Mexico / comprar Tesamorelin + Ipamorelin en México: reagent for research use (RUO) and nationwide shipping.
Tesamorelina + Ipamorelina is also searched as: Tesamorelina y Ipamorelina.
Identity and composition
Tesamorelin + Ipamorelin is a research coformulation that combines two growth hormone (GH) secretagogues with complementary mechanisms: a stabilized analog of GH-releasing factor (GHRH) and a pentapeptide agonist of the ghrelin receptor. It is studied as a tool to explore endogenous GH release. Product for research use.
There is no single chemical identity (CAS, molecular weight or formula) for the mixture; only the two peptides are documented separately:
- Tesamorelin: CAS 218949-48-5 (acetate salt 901758-09-6); approximate MW 5135.9 g/mol; formula C221H366N72O67S. Sequence: trans-3-hexenoyl-[GHRH(1-44)]-NH2. Synonyms: TH9507.
- Ipamorelin: CAS 170851-70-4; approximate MW 711.9 g/mol; formula C38H49N9O5. It is a pentapeptide: Aib-His-D-2-Nal-D-Phe-Lys-NH2. Synonym: NNC 26-0161.
The 17 mg presentation and the combination as a single product come from research-peptide suppliers, not from clinical literature; the dose ratio between the two components is not documented in peer-reviewed sources.
Mechanism of action
The coformulation seeks to simultaneously activate two complementary pathways on the pituitary somatotroph.
- Tesamorelin acts as a selective agonist of the GHRH receptor (GHRHR), activating the adenylate cyclase - cAMP - PKA pathway, which induces the synthesis and pulsatile release of endogenous GH, with secondary elevation of hepatic IGF-1 (PMID 20101189). Its N-terminal acylation (trans-3-hexenoyl group) protects the Ala-Asp bond from cleavage by dipeptidyl peptidase-IV (DPP-IV), which confers greater enzymatic stability than native GHRH.
- Ipamorelin is a selective agonist of the GH secretagogue receptor type 1a (GHSR-1a, the ghrelin receptor); its binding activates Gq/11 - phospholipase C - IP3 signaling, with calcium release and GH exocytosis (PMID 10496658).
In theory, co-activating the two pathways (GHRHR and GHSR-1a) would produce a synergistic release of GH. However, this synergy and the co-formulation as a product have not been validated in published clinical trials; all mechanistic information comes from the components studied separately.
Pharmacokinetics
The available pharmacokinetic data correspond to each component separately; there are no published data for the co-formulation.
- Tesamorelin (subcutaneous route): approximate terminal half-life of 8 minutes, low bioavailability (≤4%) and elimination by proteolysis.
- Ipamorelin: terminal half-life of approximately 2 hours, with dose-proportional kinetics and a GH peak at ~30-40 minutes after administration in healthy volunteers (PMID 10496658).
How the mixture behaves as a whole cannot be characterized from the existing literature.
Scientific evidence
The available evidence is limited and comes from the individual components, not the mixture. There is no peer-reviewed clinical literature on the tesamorelin + ipamorelin co-formulation as a single product.
- Tesamorelin has the most solid clinical backing: it was approved by the FDA (2010) for HIV-associated lipodystrophy with abdominal fat accumulation, with randomized phase III trials that observed a reduction of approximately 10.9-18% of visceral adipose tissue versus placebo, without significant perturbation of glucose at 6 months (PMID 20101189). It has also been investigated exploratorily in hepatic steatosis/NAFLD and cognitive impairment, with results considered preliminary.
- Ipamorelin was never approved; its development (Novo Nordisk/Helsinn) was halted. It reached phase II for postoperative ileus (NCT00672074), discontinued for lack of efficacy over placebo; the human evidence is limited to early pharmacokinetic/pharmacodynamic studies and that trial (PMID 10496658; NCT00672074).
Any claim of efficacy for the combination is speculative and must be interpreted as a research compound.
Research applications
Product for research use. This material is offered exclusively as a laboratory reagent.
It may be of interest for research in:
- In vitro or preclinical-model studies on the signaling of GHRHR and GHSR-1a receptors.
- Comparative characterization of GH secretagogues and their release pathways.
- Methodological work on the stability and handling of coformulated peptides.
Not applicable for:
- clinical use, therapeutic use, diagnostic or preventive.
- Administration in humans or in clinical veterinary use.
- Sports use: both peptides appear on the prohibited substances list of WADA.
Research protocols
There are no established dosing protocols for the coformulation, since there are no published clinical trials on the blend nor justification in the literature for the 17 mg presentation.
As a reference for the components separately in human studies:
- Ipamorelin was administered at 0.03 mg/kg twice a day for up to 7 days in the phase II trial of postoperative ileus, a regimen generally well tolerated but without efficacy over placebo (NCT00672074).
- Tesamorelin was evaluated in phase III trials of HIV lipodystrophy by daily subcutaneous injection (PMID 20101189).
These data correspond to clinical contexts specific to each molecule and do not constitute a guide for the combination. Any research scheme must be defined under the controls of the responsible laboratory.
Reconstitution
General standard laboratory guide for lyophilized peptides. The material is usually reconstituted with bacteriostatic water (sterile water with 0.9% benzyl alcohol) or, depending on the experimental design, with sterile water for injection.
- Add the diluent slowly along the vial wall, letting it run down onto the powder rather than directing it straight onto it.
- Do not shake; swirl or rotate the vial gently until complete dissolution to preserve the integrity of the peptide.
- Calculate the diluent volume according to the concentration desired for the experimental work.
These indications are general handling practices; they do not imply suitability for clinical use.
Stability and storage
Standard peptide handling practices.
- Lyophilized: the dry powder is more stable. It is recommended to store it protected from light, moisture, and heat; refrigerated and, for prolonged storage, frozen.
- Reconstituted: the solution is less stable and must be kept refrigerated, being used within a short period in accordance with laboratory practices.
- Avoid repeated freeze-thaw cycles, which can degrade the peptide.
No specific stability data have been published for this coformulation; these are general storage recommendations.
Safety profile
The available safety data correspond to each component separately, not to the mixture, and do not substitute for a characterization of the coformulation.
- Tesamorelin: in HIV trials it was generally well tolerated, without significant disturbance of glucose at 6 months (PMID 20101189). The FDA label warns about possible increase in IGF-1, glucose alterations/insulin resistance, injection-site reactions, and edema/arthralgias. Noted contraindications: pregnancy, active malignancy, and disruption of the pituitary axis.
- Ipamorelin: well tolerated in the phase II postoperative ileus trial (0.03 mg/kg twice daily for up to 7 days), with no relevant safety signals, although without efficacy (NCT00672074).
The interactions and long-term safety of the coformulation have not been characterized. Both peptides are on the WADA prohibited substances list. To reiterate: product for research use.
Comparative context
Within its class, each component occupies a distinct place:
- Tesamorelin differs from other GHRH analogs (such as sermorelin or CJC-1295) by its stabilization through N-terminal acylation against DPP-IV and by being the only one of the class with regulatory approval, in the specific indication of HIV-associated lipodystrophy.
- Ipamorelin belongs to the ghrelin-type peptide secretagogues (GHSR-1a) and is considered one of the most selective, with less stimulation of cortisol and prolactin than earlier secretagogues such as GHRP-6 or hexarelin.
The logic of combining a GHRHR agonist with a GHSR-1a one is analogous to experimentally studied pairs (GHRH + GHRP), but for this specific pair there are no direct comparative data.
History and development
The two components have very different development trajectories.
- Tesamorelin (TH9507) was developed as a stabilized analog of GHRH and approved by the FDA in 2010 for HIV-associated lipodystrophy with abdominal fat accumulation, supported by randomized phase III trials (PMID 20101189). It was subsequently explored in early phases in hepatic steatosis/NAFLD and cognitive impairment.
- Ipamorelin (NNC 26-0161) was developed by Novo Nordisk/Helsinn and never reached approval; its development was halted after a phase II trial in postoperative ileus that was discontinued for lack of efficacy versus placebo (NCT00672074).
La coformulation tesamorelin + ipamorelin and the 17 mg presentation do not come from the pharmaceutical development of either compound, but from the research-peptide market; there is no clinical literature supporting it as a single product.
FAQ
Is the tesamorelin + ipamorelin combination approved or clinically validated?
No. There is no peer-reviewed clinical literature on the coformulation as a single product. Tesamorelin has FDA approval (2010) only for HIV-associated lipodystrophy, while ipamorelin was never approved. The combination comes from the research peptide market and any claim of efficacy for the mixture is speculative.
How do these two peptides work together?
In theory they act on complementary pathways: tesamorelin is a GHRH receptor agonist (cAMP-PKA pathway) and ipamorelin a ghrelin receptor GHSR-1a agonist (phospholipase C-IP3 pathway). Coactivating them could produce synergistic GH release, but this synergy has not been validated in published clinical trials for this specific pair.
What is the half-life of each component?
According to data on the components separately, subcutaneous tesamorelin has a terminal half-life of approximately 26-38 minutes, and ipamorelin of around 2 hours, with a GH peak at 30-40 minutes in healthy volunteers (PMID 10496658). There are no published pharmacokinetic data for the coformulation.
Why is the presentation 17 mg and in what proportion do they come?
The 17 mg presentation and the proportion between the two components come from research-peptide suppliers, not from clinical literature. There is no published pharmacokinetic justification or a documented dose ratio in peer-reviewed sources.
How is it reconstituted and stored?
As a general laboratory practice, the lyophilizate is reconstituted with bacteriostatic water added slowly down the wall of the vial, without shaking. The dry powder is more stable and is kept refrigerated or frozen, protected from light and moisture; once reconstituted it must be refrigerated, used within a short period, and freeze-thaw cycles avoided.
Can it be used in humans or in sport?
No. It is a product for research use; not for clinical, therapeutic or diagnostic use. In addition, both peptides appear on the list of substances prohibited by the World Anti-Doping Agency (WADA).
Scientific references (5)
Peer-reviewed literature on Tesamorelin + Ipamorelin, with its PubMed identifier when available:
- Tesamorelin reduces visceral adipose tissue (Falutz J, et al. · New England Journal of Medicine · 2007) — Clinical study of tesamorelin for visceral fat reduction. PMID 18057338.
- About Ipamorelin: Ipamorelin, the first selective growth hormone secretagogue (Raun, et al. · European Journal of Endocrinology · 1998) PMID 9849822.
- About Tesamorelin: A placebo-controlled, dose-ranging study of a growth hormone releasing factor in HIV-infected patients with abdominal fat accumulation (Falutz, et al. · AIDS · 2005) PMID 16052083.
- About Ipamorelin: A new series of highly potent growth hormone-releasing peptides derived from ipamorelin (Ankersen, et al. · Journal of Medicinal Chemistry · 1998) PMID 9733495.
- About Tesamorelin: Tesamorelin: a review of its use in the management of HIV-associated lipodystrophy (Dhillon, et al. · Drugs · 2011) PMID 21668043.
Full scientific profile: Tesamorelin in the compendium — mechanism of action, studies and technical data sheet.
See the full category catalog: Hormonal · Metabolism.