Tezusomant | CAS No. 2802416-72-2 manufacturer

Description

Product Description

Tezusomant is a novel investigational growth hormone receptor antagonist (GHRA) developed to counteract the pathological effects of excessive growth hormone signaling. Growth hormone (GH) is secreted by the anterior pituitary gland and plays a pivotal role in regulating growth, metabolism, and tissue homeostasis. However, when GH is secreted in excess, as in the case of acromegaly or certain pituitary adenomas, it can lead to severe clinical manifestations, including abnormal skeletal overgrowth, metabolic disturbances, and multi-organ complications.

Tezusomant is designed to directly target the growth hormone receptor (GHR), preventing the downstream activation of signaling pathways such as JAK2/STAT5, MAPK, and PI3K-Akt. This action makes it highly effective in neutralizing the proliferative and metabolic effects of GH. By antagonizing GHR, Tezusomant inhibits the production of insulin-like growth factor-1 (IGF-1), which mediates many of GH’s growth-promoting effects.

Clinical and Research Context

The development of GHR antagonists like Tezusomant was motivated by limitations of conventional therapies for acromegaly, which typically include:

• Surgical removal of pituitary tumors – not always curative, especially in macroadenomas.

• Somatostatin analogs – effective but may not normalize IGF-1 in all patients.

• Dopamine agonists – less effective as monotherapy in severe disease.

Tezusomant provides researchers with a targeted pharmacological approach for studying GH hypersecretion disorders. Its high specificity allows detailed exploration of the role of GH and IGF-1 in:

• Skeletal growth regulation

• Glucose and lipid metabolism

• Cardiovascular health

• Tumor biology in GH-related neoplasms

Key Features

• Selective GH receptor blockade without intrinsic agonist activity.

• Potential for better IGF-1 normalization compared to existing therapies.

• Research value in both metabolic and oncological settings.

• Therapeutic promise for conditions linked to GH overexpression or resistance.

Product Specifications

Extended Notes on Specifications

• Formulation: Designed as a stable peptide analog with optimized pharmacokinetics for receptor binding studies.

• Solubility: Ready-to-use in standard physiological buffers for in vitro and in vivo experiments.

• QC Measures: Analytical validation ensures consistency across experimental batches, reducing variability in results.

• Research Use: Ideal for dissecting the endocrine and metabolic effects of GH signaling.

Mechanism of Action

The mechanism of Tezusomant is centered on competitive inhibition of GH binding to its receptor.

1. Receptor Binding Blockade

   • GH normally binds to its receptor (GHR) on hepatocytes and peripheral tissues.

   • Tezusomant binds to GHR without activating downstream signaling, effectively blocking GH from engaging the receptor.

2. Inhibition of Downstream Signaling

   • Prevents JAK2 activation, thereby suppressing STAT5 phosphorylation.

   • Downregulates transcription of IGF-1 and other GH-responsive genes.

3. Reduced IGF-1 Production

   • Hepatic IGF-1 synthesis is a key mediator of GH’s systemic effects.

   • By lowering IGF-1 levels, Tezusomant indirectly curtails tissue overgrowth and metabolic dysregulation.

4. Physiological Outcomes

   • Inhibition of abnormal bone growth (a hallmark of acromegaly).

   • Improvement in glucose tolerance by reducing GH-induced insulin resistance.

   • Cardiovascular benefits, as excessive GH/IGF-1 activity has been linked to cardiomyopathy.

Broader Research Applications

• Metabolism: Useful in exploring how GH influences adiposity, lipid metabolism, and diabetes.

• Oncology: IGF-1 axis plays a role in tumor progression; Tezusomant aids in dissecting this relationship.

• Aging Research: GH and IGF-1 are implicated in longevity and age-related diseases; antagonists provide insights into lifespan modulation.

  

Side Effects

While Tezusomant is primarily a research-use-only compound, knowledge from similar GH receptor antagonists suggests several possible outcomes that researchers should monitor.

Potential Adverse Reactions (Research Context)

• Injection site reactions (erythema, irritation in in vivo studies).

• Altered glucose metabolism – excessive antagonism may lead to hypoglycemia in experimental models.

• Liver enzyme elevations – some GHR antagonists show mild hepatotoxicity in clinical analogs.

• IGF-1 deficiency effects – prolonged blockade may result in fatigue, muscle weakness, or reduced bone density in animal models.

Laboratory Safety Considerations

• Use protective equipment when handling.

• Store under recommended conditions to preserve bioactivity.

• Dispose of waste in compliance with peptide handling protocols.

Long-Term Considerations

Chronic suppression of GH/IGF-1 signaling has complex systemic effects. Researchers studying aging, cancer, or metabolic disease must carefully balance dose and exposure time to model physiological versus pathological conditions.

Disclaimer

For research use only. Not for human, veterinary, or clinical use.

Keywords

Tezusomant, growth hormone receptor antagonist, GHRA, acromegaly research, growth hormone signaling, IGF-1 inhibitor, endocrine research compound.peptide manufacturer

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