Tesamorelin is a synthetic analog of growth hormone-releasing hormone (GHRH) designed with structural modifications to enhance stability and resistance to enzymatic degradation. It acts as a selective agonist of the GHRH receptor, stimulating the release of endogenous growth hormone (GH) from the anterior pituitary. Tesamorelin is widely used in research involving GH secretion, lipid metabolism, and the regulation of the GH/IGF-1 axis.
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Questions
Tesamorelin Common Questions
What’s pIC50?
pIC50 is the negative log of the IC50 value when converted to molar.That is, pIC50=-log(IC50).
What’s Kd?
Dissociation consent (Kd) reflects the affinity of a compound for its target. In some cases, it can be equivalent to Ki.
Description
Tesamorelin is a synthetic analog of growth hormone-releasing hormone (GHRH) designed with structural modifications to enhance stability and resistance to enzymatic degradation. It acts as a selective agonist of the GHRH receptor, stimulating the release of endogenous growth hormone (GH) from the anterior pituitary. Tesamorelin is widely used in research involving GH secretion, lipid metabolism, and the regulation of the GH/IGF-1 axis.
Targets & IC50
Targets:
Growth Hormone-Releasing Hormone Receptor (GHRHR)
cAMP Signaling Pathway
GH/IGF-1 Axis
IC50:
Not applicable (Tesamorelin is a receptor agonist peptide, not an inhibitory compound)
In vitro
METHODS: Primary anterior pituitary cells and rat pituitary cell lines were treated with Tesamorelin (0–100 nM) for 1–24 hours. Growth hormone secretion and intracellular signaling were evaluated using ELISA assays and cAMP measurements.
RESULTS: Tesamorelin stimulates growth hormone secretion in a dose-dependent manner via activation of the GHRH receptor. It increases intracellular cAMP levels and enhances pulsatile GH release. Compared to native GHRH, Tesamorelin demonstrates improved stability and prolonged activity while maintaining receptor specificity. No significant cytotoxicity is observed at commonly used experimental concentrations. [1]
Synonyms
GHRH analog Tesamorelin
Molecular Weight
5135.9 Da
Formula
C₂₂₁H₃₆₆N₇₂O₆₇ (approximate)
Cas No.
218949-48-5
Smiles
Not applicable (peptide)
Relative Density.
no data available
Sequence
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-Leu-Ser-Arg-Leu-Ala
Sequence Short
30 aa
Storage
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