Description

Product Description

Axareotide (CAS 2126833-17-6) is a synthetic somatostatin analogue peptide designed to mimic the biological effects of endogenous somatostatin, a key regulatory hormone involved in inhibiting endocrine secretion, modulating neurotransmission, and controlling cell proliferation. Somatostatin acts through five G protein–coupled receptor subtypes (SSTR1–SSTR5), which are distributed in a wide range of tissues, including the pituitary gland, pancreas, gastrointestinal tract, and nervous system.

Axareotide selectively binds to multiple somatostatin receptor subtypes, particularly SSTR2 and SSTR5, with high affinity, triggering Gi protein–mediated signaling cascades that suppress adenylyl cyclase activity and decrease intracellular cyclic AMP (cAMP) levels. This inhibitory signaling reduces the secretion of key hormones such as growth hormone (GH), insulin, glucagon, gastrin, and thyroid-stimulating hormone (TSH), thereby providing an effective molecular tool for research into neuroendocrine control and metabolic regulation.

In oncological studies, Axareotide has been employed to investigate the antiproliferative properties of somatostatin analogues. Activation of somatostatin receptors leads to cell cycle arrest, induction of apoptosis, and inhibition of angiogenesis through the downregulation of vascular endothelial growth factor (VEGF). The peptide’s receptor-binding versatility makes it valuable in preclinical research on neuroendocrine tumors, pituitary adenomas, and gastrointestinal carcinoids.

In neuroscience research, Axareotide has been utilized to explore somatostatin’s neuromodulatory role in the central nervous system. Somatostatin receptor activation influences synaptic transmission, neuronal excitability, and neuroprotection through the regulation of calcium channel activity and membrane hyperpolarization.

Pharmacologically, Axareotide exhibits improved enzymatic stability and receptor selectivity compared with natural somatostatin, providing longer biological activity in experimental systems. Its stability allows for sustained receptor activation, making it ideal for in vitro receptor pharmacology, signaling pathway dissection, and peptide–receptor binding kinetics studies.

Collectively, Axareotide is a research-grade somatostatin mimetic that supports a wide spectrum of investigations in endocrine signaling, metabolic regulation, neuroendocrine oncology, and pharmacodynamic receptor mapping.

Product Specifications

Mechanism of Action

Axareotide acts as a potent agonist at somatostatin receptors (SSTR1–SSTR5), particularly SSTR2 and SSTR5. These receptors belong to the G protein–coupled receptor (GPCR) family and primarily mediate inhibitory signals through Gi/o proteins. Upon receptor engagement, Axareotide induces adenylyl cyclase inhibition, leading to reduced cAMP synthesis and downstream suppression of protein kinase A (PKA) activity.

This signaling pathway results in the inhibition of voltage-gated calcium channels, decreasing calcium influx and suppressing exocytosis of secretory granules. Consequently, secretion of key hormones—such as growth hormone, insulin, glucagon, and gastrin—is attenuated.

In addition to hormonal control, Axareotide activation of somatostatin receptors exerts antiproliferative and antiangiogenic effects via activation of protein tyrosine phosphatases (PTPs) and modulation of MAPK and PI3K/Akt pathways. These molecular effects contribute to reduced tumor cell growth, migration, and vascularization in various cancer models.

Axareotide also affects neuronal signaling by promoting potassium channel opening, causing membrane hyperpolarization and decreased excitatory neurotransmission. This underlies its use in research on neurotransmitter modulation and neuronal network inhibition.

Overall, Axareotide’s mechanism provides a valuable experimental system for understanding hormone feedback loops, signal transduction cascades, and tumor suppression mechanisms governed by the somatostatin receptor family.

Side Effects

In laboratory settings, Axareotide demonstrates a low toxicity profile, but exaggerated receptor stimulation may transiently alter glucose metabolism, hormone levels, or cellular signaling balance. In vitro exposure at high concentrations can reduce cell proliferation or induce mild apoptotic activity due to prolonged somatostatin receptor activation.

Potential reversible effects observed in animal models include temporary reduction in growth hormone levels, mild hypoglycemia, or decreased gastrointestinal motility. These findings underscore the importance of dose optimization when using Axareotide in preclinical systems.

No genotoxic or mutagenic properties have been reported. The compound is for research use only, not for human or therapeutic administration.

Disclaimer

All information provided is intended for laboratory research use only. Axareotide is not approved for diagnostic or therapeutic applications.

Keywords

Axareotide, CAS 2126833-17-6, somatostatin analogue, SSTR agonist, endocrine peptide, neuroendocrine tumor research, hormone secretion inhibitor, GPCR modulator, peptide pharmacology compound

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