Tesamorelin & Ipamorelin Blend (8mg)

$90.00

Tesamorelin & Ipamorelin blend is Synthesized and Lyophilized in the USA.

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Description

Tesamorelin & Ipamorelin Peptide Blend

The Tesamorelin & Ipamorelin peptide blend is a mixture of peptide compounds that have been studied for their possible interaction with certain receptors in the cells of the pituitary gland. These receptors include the growth-hormone secretagogue (GHS) receptors and growth hormone-releasing hormone (GHRH) receptors, which are associated with the release of growth hormone (HGH).

Tesamorelin, which is a synthetic peptide, is believed by researchers to act as an analog of growth hormone-releasing hormone through binding to GHRH receptors.[1] Tesamorelin consists of an amino acid chain with 44 amino acids, including a specific sequence similar to GHRH. Additionally, Tesamorelin appears to have been modified to potentially enhance its resistance to enzymatic degradation. As an example, the C-terminus of the synthetically developed Tesamorelin has been modified with a trans-3-hexenoic acid group. This modification, known as an omega-amino acid modification, may help improve the peptide’s resistance to enzymatic degradation.

Tesamorelin also has an acetyl group (CH₃CO-) attached to its N-terminus, which may potentially enhance the stability and bioactivity of the peptide. As a result, the peptide is also known as N-(trans-3-hexenoyl)-[Tyr1]hGRF(1–44)NH2 acetate.[2] By interacting with GHRH receptors in the pituitary and hypothalamus, Tesamorelin may trigger the release of HGH from pituitary cells.

Similarly, Ipamorelin is also a synthetic peptide that interacts with pituitary cells and may stimulate the synthesis and release of HGH. Its proposed mechanism of action involves interaction with GHS receptors, also known as ghrelin receptors, which are found in the pituitary and hypothalamus.[3] By activating these receptors, Ipamorelin may mimic the effects of ghrelin on the pituitary gland, potentially leading to the release of growth hormone from pituitary cells.

Specifications

Tesamorelin Molecular Formula: C223H370N72O69S

Ipamorelin Molecular Formula: C38H49N9O5

Tesamorelin Molecular Weight: 5195.908 g/mol

Ipamorelin Molecular Weight: 711.868 g/mol

Tesamorelin Sequence: YADAIFTNSYRKVLGQLSARKLLQDIMSRQQGESNQERGARARL

Ipamorelin Sequence: Aib-His-D-2Nal-D-Phe-Lys

Tesamorelin & Ipamorelin Peptide Blend Research

Tesamorelin & Ipamorelin and the Pituitary Gland
As suggested, Tesamorelin may interact with the pituitary gland by potentially binding to the GHRH receptors, which may initiate a series of molecular events.[4] Researchers suggest that should Tesamorelin bind to the GHRH receptor, it may cause structural changes in the receptor, activating intracellular signaling pathways.[5] The researchers comment that the binding process “is followed by a major conformational change that involves a large kink at the TM6 to open the intracellular face for G protein coupling.” One possible pathway appears to involve the apparent stimulation of cyclic adenosine monophosphate (cAMP) production within pituitary cells. This may possibly be achieved by activating the enzyme adenylate cyclase, which may convert ATP to cAMP. It is posited by researchers that increased cAMP levels may activate protein kinase A (PKA), which is hypothesized to be an important intracellular signaling molecule. PKA may potentially phosphorylate various target proteins, possibly initiating cellular responses. This proposed activation of the GHRH receptor by Tesamorelin and the subsequent cAMP-PKA signaling cascade may stimulate the synthesis and secretion of growth hormone (HGH) from somatotrophs in the pituitary gland.

On the other hand, it appears that Ipamorelin may exhibit selectivity towards the GHS receptor without purportedly having significant interaction with other receptors or affecting the release of other mediators, such as adrenocorticotropic hormone (ACTH) and cortisol.[6] By possibly binding to the GHS receptors, Ipamorelin appears to activate various intracellular signaling pathways.[7] One potential pathway appears to involve the activation of phospholipase C (PLC), which might lead to the release of inositol triphosphate (IP3) and diacylglycerol (DAG). IP3 may potentially trigger the release of calcium ions (Ca2+) from intracellular stores, while DAG potentially activates protein kinase C (PKC). The elevation of intracellular calcium levels and potential PKC activation may result in the exocytosis of growth hormone-containing vesicles from pituitary cells.

Tesamorelin & Ipamorelin Blend and the Musculoskeletal System
One study analyzed the impact of Tesamorelin on muscle tissue quality.[8] The researchers employed computed tomography (CT) scans to measure muscle density and area before and after introducing Tesamorelin or a placebo. The trial study suggested that Tesamorelin may be associated with muscle density and area improvements. The potential of Tesamorelin may be especially noticeable in certain types of muscles, such as rectus abdominis, psoas major, and paraspinal muscles. These improvements were reflected by increased muscle density and area or decreased fat content in these muscle groups. The changes were statistically significant compared to the placebo group. But even though Tesamorelin is considered to act through other molecules such as insulin-like growth factor-1 (IGF-1), no significant correlation was observed between changes in IGF-1 levels and changes in muscle density or area.

Preliminary studies using experimental models suggest that Ipamorelin might exhibit actions that resemble those observed in Tesamorelin on skeletal muscle and bone. However, these findings have not been fully confirmed.[9] More specifically, Ipamorelin appeared to interact with and potentially raise insulin-like growth factor-I (IGF-I) levels. These actions appeared to be associated with increased muscle fiber size, muscle mass, and an enhancement in skeletal muscle strength in this murine trial. Notably, Ipamorelin also appeared to exhibit positive action on bone health, possibly stimulating bone formation and promoting an increase in bone mass. The study further observed an apparent increase in bone mineral content, potentially associated with Ipamorelin. Ipamorelin’s favorable potential on bone tissue has also been suggested by other murine trials.[10] [11] One of the murine trials investigated the potential of Ipamorelin on bone mineral content (BMC). The scientists suggested that there could be an increase in the test animals’ body weight and BMC, as potentially measured by dual X-ray absorptiometry (DXA). However, when adjusted for the increase in body weight, the ratio of BMC to body weight appeared to remain unaffected. An in vitro analysis also suggested that the increase in cortical BMC may potentially result from an increase in bone area. At the same time, the volumetric BMD may potentially remain unchanged. The scientists commented that “the results of in vitro measurements using pQCT and Archimedes’ principle, in addition to ash weight determinations, show that the increases in cortical and total BMC were due to an increased growth of the bones with increased bone dimensions, whereas the volumetric BMD was unchanged.

Disclaimer: The products mentioned are not intended for human or animal consumption. Research chemicals are intended solely for laboratory experimentation and/or in-vitro testing. Bodily introduction of any sort is strictly prohibited by law. All purchases are limited to licensed researchers and/or qualified professionals. All information shared in this article is for educational purposes only.

 

References

  1. Clinical Review Report: Tesamorelin (Egrifta) [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2016 Aug. 1, Introduction. Available from: https://www.ncbi.nlm.nih.gov/books/NBK539137/
  2. Ferdinandi, E. S., Brazeau, P., High, K., Procter, B., Fennell, S., & Dubreuil, P. (2007). Non-clinical pharmacology and safety evaluation of TH9507, a human growth hormone-releasing factor analogue. Basic & clinical pharmacology & toxicology, 100(1), 49–58. https://doi.org/10.1111/j.1742-7843.2007.00008.x
  3. Johansen, P. B., Nowak, J., Skjaerbaek, C., Flyvbjerg, A., Andreassen, T. T., Wilken, M., & Orskov, H. (1999). Ipamorelin, a new growth-hormone-releasing peptide, induces longitudinal bone growth in rats. Growth hormone & IGF research : official journal of the Growth Hormone Research Society and the International IGF Research Society, 9(2), 106–113. https://doi.org/10.1054/ghir.1999.9998
  4. Spooner, L. M., & Olin, J. L. (2012). Tesamorelin: a growth hormone-releasing factor analogue for HIV-associated lipodystrophy. The Annals of pharmacotherapy, 46(2), 240–247. https://doi.org/10.1345/aph.1Q629
  5. Zhou, F., Zhang, H., Cong, Z., Zhao, L. H., Zhou, Q., Mao, C., Cheng, X., Shen, D. D., Cai, X., Ma, C., Wang, Y., Dai, A., Zhou, Y., Sun, W., Zhao, F., Zhao, S., Jiang, H., Jiang, Y., Yang, D., Eric Xu, H., … Wang, M. W. (2020). Structural basis for activation of the growth hormone-releasing hormone receptor. Nature communications, 11(1), 5205. https://doi.org/10.1038/s41467-020-18945-0
  6. Raun, K., Hansen, B. S., Johansen, N. L., Thøgersen, H., Madsen, K., Ankersen, M., & Andersen, P. H. (1998). Ipamorelin, the first selective growth hormone secretagogue. European journal of endocrinology, 139(5), 552–561. https://doi.org/10.1530/eje.0.1390552
  7. Jiménez-Reina, L., Cañete, R., de la Torre, M. J., & Bernal, G. (2002). Influence of chronic treatment with the growth hormone secretagogue Ipamorelin, in young female rats: somatotroph response in vitro. Histology and histopathology, 17(3), 707–714. https://doi.org/10.14670/HH-17.707
  8. Adrian, S., Scherzinger, A., Sanyal, A., Lake, J. E., Falutz, J., Dubé, M. P., Stanley, T., Grinspoon, S., Mamputu, J. C., Marsolais, C., Brown, T. T., & Erlandson, K. M. (2019). The Growth Hormone Releasing Hormone Analogue, Tesamorelin, Decreases Muscle Fat and Increases Muscle Area in Adults with HIV. The Journal of frailty & aging, 8(3), 154–159. https://doi.org/10.14283/jfa.2018.45
  9. Andersen, N. B., Malmlöf, K., Johansen, P. B., Andreassen, T. T., Ørtoft, G., & Oxlund, H. (2001). The growth hormone secretagogue ipamorelin counteracts glucocorticoid-induced decrease in bone formation of adult rats. Growth hormone & IGF research : official journal of the Growth Hormone Research Society and the International IGF Research Society, 11(5), 266–272. https://doi.org/10.1054/ghir.2001.0239
  10. Johansen, P. B., Nowak, J., Skjaerbaek, C., Flyvbjerg, A., Andreassen, T. T., Wilken, M., & Orskov, H. (1999). Ipamorelin, a new growth-hormone-releasing peptide, induces longitudinal bone growth in rats. Growth hormone & IGF research : official journal of the Growth Hormone Research Society and the International IGF Research Society, 9(2), 106–113. https://doi.org/10.1054/ghir.1999.9998
  11. Svensson, J., Lall, S., Dickson, S. L., Bengtsson, B. A., Rømer, J., Ahnfelt-Rønne, I., Ohlsson, C., & Jansson, J. O. (2000). The GH secretagogues ipamorelin and GH-releasing peptide-6 increase bone mineral content in adult female rats. The Journal of endocrinology, 165(3), 569–577. https://doi.org/10.1677/joe.0.1650569
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