Description

Product Description

Siponimod (CAS 1230487-00-9) is a second-generation sphingosine-1-phosphate (S1P) receptor modulator, specifically designed to selectively target the S1P₁ and S1P₅ receptor subtypes. It plays a crucial role in neuroimmunological research by modulating lymphocyte egress from lymphoid tissues, thereby influencing immune cell trafficking and central nervous system (CNS) immune surveillance.

As a small-molecule compound derived from structural optimization of fingolimod, Siponimod offers enhanced receptor selectivity and a more predictable pharmacokinetic profile. It binds selectively to S1P₁ and S1P₅ receptors, sparing other S1P receptor subtypes such as S1P₂, S1P₃, and S1P₄, which are often associated with adverse cardiovascular effects. This makes Siponimod particularly valuable in mechanistic studies focused on immune modulation, neuronal signaling, and demyelination models.

In neurobiology, Siponimod serves as a potent chemical probe for evaluating the functional role of S1P signaling in neural repair, oligodendrocyte survival, and remyelination processes. By targeting S1P₁ receptors on lymphocytes, the compound reduces their migration into the CNS, effectively suppressing inflammatory cascades involved in neurodegeneration. Furthermore, S1P₅ receptor activation promotes oligodendrocyte maturation and myelin sheath stability, which are critical aspects of regenerative neuroscience.

From a molecular pharmacology perspective, Siponimod’s selective action on S1P₁/₅ receptors enables researchers to dissect downstream pathways such as ERK1/2, Akt, and Rac signaling, which are implicated in both immune and neuronal cell dynamics. These insights contribute to a deeper understanding of sphingolipid receptor biology and its relevance to autoimmune and degenerative diseases.

Its well-characterized pharmacodynamic properties, oral bioavailability, and defined metabolic pathways (CYP2C9 and CYP3A4 mediated) make Siponimod an ideal candidate for preclinical studies, receptor binding assays, and CNS distribution analyses. The compound’s stability and solubility also facilitate formulation studies and receptor-binding kinetics research, allowing precise evaluation of dose-dependent receptor modulation.

In summary, Siponimod serves as a powerful research tool in the fields of neuroimmunology, sphingolipid metabolism, and receptor pharmacology. It provides a selective, stable, and high-purity model compound for elucidating the role of S1P signaling in immune regulation and neural repair mechanisms.

Product Specifications

Mechanism of Action

Siponimod functions as a selective modulator of the sphingosine-1-phosphate receptors S1P₁ and S1P₅, which are G-protein-coupled receptors that mediate cell migration, proliferation, and survival. S1P receptors are distributed across various immune and neural tissues, and their activation plays an integral role in regulating immune cell trafficking and CNS homeostasis.

1. S1P₁ Receptor Modulation and Lymphocyte Trafficking

The S1P₁ receptor is highly expressed on lymphocytes and endothelial cells, controlling the egress of immune cells from secondary lymphoid organs into circulation. Siponimod binds to S1P₁, inducing receptor internalization and functional antagonism. This prevents lymphocytes from leaving the lymph nodes, reducing their infiltration into the CNS and other inflamed tissues.
In research settings, this mechanism allows scientists to observe how modulation of immune cell migration can alter neuroinflammatory conditions, autoimmune progression, and peripheral immune responses.

2. S1P₅ Receptor Activation in the Central Nervous System

S1P₅ receptors are predominantly expressed on oligodendrocytes and certain neural cell types. Siponimod’s agonistic effect on these receptors promotes cell survival, differentiation, and myelin maintenance. Experimental data indicate that S1P₅ activation supports remyelination and axonal protection in demyelinating disease models, such as those used in multiple sclerosis research.

3. Downstream Signaling Pathways

Through its receptor interactions, Siponimod influences multiple intracellular pathways:

• ERK1/2 and Akt pathways: Enhance cell survival and proliferation.

• Rac and Rho GTPases: Regulate cytoskeletal dynamics and cell motility.

• NF-κB and STAT signaling: Modulate immune and inflammatory responses.

• Ca²⁺ mobilization: Affects both neural excitability and immune cell activation.

Collectively, these pathways make Siponimod an excellent molecular probe for dissecting signal transduction events associated with S1P receptor modulation in both the immune and nervous systems.

Side Effects

In research and experimental contexts, Siponimod exhibits pharmacological effects related to its modulation of S1P receptors. While laboratory studies are not conducted in humans, documented data from preclinical and reference studies provide insight into potential off-target or receptor-mediated phenomena. Understanding these effects is essential for interpreting biological outcomes in experimental systems.

1. Cardiovascular Effects:
   At supraphysiological concentrations, Siponimod may transiently affect heart rate due to partial activation of S1P₁ receptors on cardiac myocytes. These effects are generally reversible and dose-dependent, illustrating receptor specificity within cardiovascular tissues.

2. Lymphocyte Reduction:
   By preventing lymphocyte egress from lymphoid tissues, the compound can lead to temporary lymphopenia in animal models. This immunomodulatory property is central to its mechanism but must be considered when designing immunological assays.

3. Liver Enzyme Fluctuations:
   In hepatocyte cultures and in vivo models, minor and reversible elevations in transaminase activity have been observed. These changes are typically associated with S1P signaling modulation and not with direct hepatotoxicity.

4. Ocular and Neurological Considerations:
   Studies using animal retinal models indicate that excessive S1P receptor activation may influence retinal vascular tone and barrier function. This makes Siponimod a useful research tool for exploring neurovascular coupling mechanisms.

5. Metabolic and CNS Effects:
   At higher concentrations, Siponimod may alter glucose metabolism, lipid signaling, and CNS neurotransmission. These findings help elucidate the systemic roles of S1P pathways in metabolic and neuronal homeostasis.

6. General Laboratory Precautions:
   Researchers should handle the compound with care, using appropriate protective measures and controlled dosing strategies. Proper documentation of dosage, exposure time, and cell line or animal strain is critical for reproducibility and data integrity.

Keywords

Siponimod, CAS 1230487-00-9, sphingosine-1-phosphate receptor modulator, S1P₁ agonist, S1P₅ agonist, lymphocyte trafficking inhibitor, neuroimmunology compound, receptor pharmacology, multiple sclerosis research, sphingolipid signaling, high-purity compound, neuroinflammation studies, CNS receptor modulator, research chemical supplier, bulk peptide and compound manufacturer China.

Shipping Guarantee

All Siponimod shipments are handled using validated cold-chain logistics to preserve compound integrity. Each package is sealed in moisture-proof containers with secondary protective wrapping and continuous temperature monitoring. Products are shipped via express international couriers with full tracking and insurance coverage.

Trade Assurance

We Siponimod ensure product authenticity, verified ≥99% purity, and compliance with analytical standards (HPLC, MS, and NMR). Each batch is supplied with a Certificate of Analysis (CoA). Our trade assurance policy guarantees replacement or refund for any deviation from listed specifications.

Payment Support

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Disclaimer

All Siponimod products listed are intended for laboratory research use only and not for human or veterinary use. They are not drugs, medical devices, or diagnostics and should not be administered to humans or animals. Researchers must handle all materials in accordance with institutional biosafety and chemical safety guidelines. The information provided is for scientific reference only and does not imply therapeutic efficacy, safety, or regulatory approval.