Description

Product Description

Motixafortide (CAS: 1447754‑15‑9) is a chemically synthesized, high-purity CXCR4 receptor antagonist designed for molecular and cellular research applications. As a potent and selective inhibitor of the C-X-C chemokine receptor type 4 (CXCR4), Motixafortide provides researchers with a robust tool for probing receptor-mediated signaling pathways, cellular chemotaxis, and molecular interactions in vitro. The compound is particularly valuable in studies focused on chemokine receptor biology, receptor-ligand binding dynamics, and downstream signal transduction mechanisms, enabling high-resolution mechanistic insights at the molecular and cellular levels.

Motixafortide operates by binding to CXCR4 with nanomolar affinity, effectively stabilizing the receptor in an inactive conformation and competitively preventing interaction with its natural ligand, stromal cell-derived factor-1α (SDF-1α/CXCL12). This inhibition allows researchers to selectively modulate CXCR4-mediated pathways, such as PI3K/AKT and MAPK/ERK signaling cascades, in controlled in vitro environments. By providing sustained receptor occupancy over extended periods, Motixafortide ensures reproducible experimental outcomes, making it suitable for detailed mechanistic analyses, receptor pharmacology studies, and high-throughput in vitro screening assays.

Structurally, Motixafortide is a cyclic peptide-based molecule with strategically positioned cationic residues that form electrostatic interactions with acidic residues within the CXCR4 binding pocket. The cyclic architecture restricts conformational flexibility, stabilizing the receptor in a non-activated state and enhancing selectivity for CXCR4 over other chemokine receptors. This combination of high affinity, prolonged receptor occupancy, and molecular specificity makes Motixafortide a preferred reagent for studying receptor-ligand dynamics and signal transduction in vitro.

In addition to its role in receptor-focused research, Motixafortide has been widely utilized in cellular migration studies. It enables researchers to investigate the molecular determinants of chemokine-directed migration, adhesion, and intracellular signaling in diverse cell types under controlled laboratory conditions. The compound is compatible with multiple in vitro experimental systems, including monolayer cultures, three-dimensional spheroid models, and co-culture assays, offering versatile applications across mechanistic, pharmacological, and cell biology studies.

High-purity Motixafortide is manufactured under strict laboratory-grade quality standards by a Chinese factory, ensuring consistent batch-to-batch reproducibility and chemical stability. It is supplied as a white to off-white powder with ≥99% purity, making it suitable for mechanistic and molecular studies requiring precise dosing and controlled experimental conditions. Researchers can access both small-scale and bulk quantities, facilitating long-term experimental projects and large-scale in vitro studies.

Motixafortide is intended exclusively for in vitro and molecular-level research. It is not for human, animal, or clinical use.

By combining potent CXCR4 antagonism, structural stability, and high purity, Motixafortide provides a reliable and effective tool for dissecting chemokine receptor biology, elucidating signaling mechanisms, and advancing fundamental molecular research. Its comprehensive applicability across receptor binding, signaling analysis, and cellular migration assays makes it an indispensable reagent for laboratories focused on chemokine-mediated processes and in vitro molecular pharmacology.

Product Specifications

Mechanism of Action

Motixafortide is a highly selective CXCR4 receptor antagonist, acting through competitive inhibition of the natural ligand SDF-1α (CXCL12) in controlled in vitro settings. The C-X-C chemokine receptor type 4 (CXCR4) plays a critical role in cellular signaling, migration, and chemotactic responses, making it a central target for mechanistic studies in molecular and cellular biology. By binding with nanomolar affinity, Motixafortide stabilizes CXCR4 in an inactive conformation, effectively preventing receptor activation and downstream signal propagation.

At the molecular level, Motixafortide interacts with multiple residues within the CXCR4 binding pocket. Its cationic amino acid residues form electrostatic interactions with negatively charged receptor sites, while the cyclic peptide structure imposes conformational constraints that enhance binding specificity. This structural arrangement not only increases receptor selectivity but also prolongs receptor occupancy, allowing sustained inhibition of CXCR4-mediated pathways in vitro.

The blockade of CXCR4 by Motixafortide disrupts key intracellular signaling cascades, including PI3K/AKT, MAPK/ERK, and other chemokine-regulated pathways. These pathways are fundamental to cell migration, adhesion, and cytoskeletal rearrangements. By modulating these mechanisms, Motixafortide enables researchers to dissect chemokine receptor-dependent molecular events with high precision. Additionally, the compound’s ability to maintain long-term receptor occupancy facilitates kinetic studies of receptor-ligand interactions, dose-response analysis, and mechanistic modeling in cellular systems.

Motixafortide is particularly effective in in vitro models that require controlled modulation of CXCR4 activity, such as migration assays, receptor-binding studies, and signaling pathway analyses. Its high specificity ensures minimal off-target effects, allowing accurate interpretation of CXCR4-mediated processes. Researchers can utilize Motixafortide to investigate receptor internalization, ligand-binding dynamics, and pathway cross-talk within complex cellular environments, including monolayer cultures, co-culture systems, and three-dimensional cell models.

In summary, Motixafortide functions as a potent, high-affinity CXCR4 antagonist that stabilizes the receptor in an inactive state, blocks ligand-induced signaling, and modulates downstream molecular pathways. Its chemical structure and receptor-binding characteristics provide a reliable and reproducible tool for in vitro mechanistic studies, receptor pharmacology research, and cellular migration investigations. Motixafortide’s role as a research reagent is limited to controlled laboratory environments, ensuring that insights into CXCR4 signaling and chemokine-mediated processes can be achieved without in vivo application.

Applications

Motixafortide is primarily applied as a high-affinity CXCR4 antagonist in in vitro research to explore chemokine receptor biology, signaling pathways, and cellular migration processes. Its specificity and prolonged receptor occupancy make it an indispensable tool for mechanistic studies that require precise modulation of CXCR4 activity. Researchers utilize Motixafortide in diverse laboratory applications, ranging from receptor-ligand interaction assays to signal transduction and chemotaxis studies.

One of the primary applications of Motixafortide is in receptor binding and affinity assays. By competing with the natural ligand SDF-1α/CXCL12 for CXCR4 binding, Motixafortide allows researchers to quantitatively measure receptor-ligand interactions, analyze binding kinetics, and evaluate receptor occupancy under controlled experimental conditions. These studies are critical for understanding the molecular determinants of chemokine recognition and for mapping the structural features required for receptor modulation.

Motixafortide is also widely used in cell migration and chemotaxis assays. In vitro systems, such as Transwell migration or wound healing (scratch) assays, benefit from Motixafortide’s ability to inhibit CXCR4-mediated signaling, allowing researchers to dissect the molecular mechanisms governing chemokine-directed cell movement. These studies are particularly relevant for understanding the intracellular signaling events that control cytoskeletal rearrangements, directional migration, and adhesion processes.

Additionally, Motixafortide serves as a key reagent for signal transduction research. By blocking CXCR4 activation, it enables the detailed study of downstream pathways, including PI3K/AKT, MAPK/ERK, and other chemokine-regulated signaling cascades. Researchers can investigate phosphorylation events, protein-protein interactions, and pathway crosstalk in various in vitro models, providing insights into the mechanistic roles of CXCR4 in cellular processes.

Motixafortide is compatible with multiple cell culture systems, including monolayer cultures, co-culture assays, and three-dimensional (3D) spheroid models. Its versatility allows integration with high-content imaging, proteomics, and transcriptomics studies, enabling comprehensive mechanistic analyses. Furthermore, Motixafortide can be applied in experimental designs incorporating multi-omics approaches, computational modeling, or receptor-ligand simulation studies to deepen understanding of CXCR4-mediated signaling networks.

In summary, Motixafortide is a robust, high-purity research reagent that provides precise, reproducible control over CXCR4 activity in vitro. Its applications encompass receptor binding studies, chemotaxis assays, signal transduction analysis, and multi-omic mechanistic investigations, making it an essential tool for laboratories exploring chemokine receptor biology, molecular signaling pathways, and cell migration mechanisms.

Research Models

Motixafortide is a versatile tool for in vitro research and can be applied across a wide range of experimental models to study CXCR4 receptor biology, signal transduction, and chemokine-mediated cellular processes. Its high specificity and prolonged receptor occupancy enable precise mechanistic investigations in controlled laboratory settings, making it suitable for both basic and advanced molecular research.

Cell Line Models

Motixafortide is widely used in mammalian cell lines that express CXCR4, including human-derived and other vertebrate cell systems. These models allow researchers to study receptor-ligand interactions, receptor internalization, and downstream signaling events. Stable or transient CXCR4-expressing cell lines are particularly useful for investigating the impact of Motixafortide on chemokine-directed signaling pathways, including PI3K/AKT and MAPK/ERK cascades, and for dissecting molecular mechanisms of receptor regulation.

3D Culture Systems

In addition to traditional monolayer cultures, Motixafortide is compatible with three-dimensional (3D) culture models, such as spheroids or organoids. These models provide a more physiologically relevant environment for studying cell migration, adhesion, and receptor-mediated signaling dynamics. By applying Motixafortide in 3D cultures, researchers can assess how CXCR4 antagonism influences cellular behavior in a context that better mimics tissue architecture and multicellular interactions.

Co-Culture and Multi-Cell Models

Motixafortide is also suitable for co-culture systems, where two or more cell types are studied simultaneously to investigate paracrine signaling or cell-cell interactions mediated by CXCR4. These models allow mechanistic analysis of how Motixafortide modulates chemokine gradients, intercellular communication, and receptor-dependent signal transduction in complex cellular networks.

Integrative Models

For laboratories combining in vitro research with multi-omic and computational approaches, Motixafortide can be incorporated into models for proteomics, transcriptomics, and metabolomics studies. Computational modeling and molecular docking simulations can further elucidate receptor-ligand interactions and predict the effects of CXCR4 inhibition, providing complementary insights to experimental data.

Summary

Overall, Motixafortide provides a high-purity, reliable reagent for a variety of in vitro research models. Its application spans conventional monolayer cell cultures, advanced 3D models, co-culture systems, and integrative multi-omic studies. By enabling controlled modulation of CXCR4 activity, Motixafortide facilitates detailed mechanistic analysis of chemokine receptor signaling, migration processes, and molecular pathway regulation, making it an essential tool for mechanistic research at the cellular and molecular levels.

Motixafortide is strictly for research purposes in vitro and at the molecular level and is not intended for human, animal, or clinical use.

Experimental Design Considerations

When planning in vitro studies with Motixafortide, careful experimental design is essential to ensure reproducible and mechanistically informative results. Motixafortide’s high affinity and selective antagonism of CXCR4 allow researchers to dissect receptor-mediated signaling pathways, cell migration mechanisms, and receptor-ligand interactions under controlled laboratory conditions.

Dose Selection and Optimization

Selecting appropriate concentrations is critical for achieving meaningful in vitro results. Based on reported IC₅₀ values (0.42–4.5 nM for CXCR4), initial dose-response experiments are recommended to identify the effective concentration range for your specific cell line or assay system. Gradual titration of Motixafortide concentrations can provide insights into receptor occupancy, potency, and potential saturation effects, ensuring accurate mechanistic interpretation.

Timing and Exposure

Motixafortide exhibits prolonged receptor occupancy, allowing extended inhibition of CXCR4-mediated pathways in vitro. Researchers should carefully plan the duration of exposure to match the kinetics of their experimental system, whether for short-term receptor binding assays, intermediate-term migration studies, or longer-term signaling pathway analyses. Maintaining stable concentrations over the intended exposure period ensures consistent receptor inhibition and reproducible results.

Assay Selection

Motixafortide is compatible with a variety of in vitro assays, including receptor binding studies, chemotaxis assays (e.g., Transwell migration or scratch assays), and downstream signaling analyses such as phosphorylation of PI3K/AKT and MAPK/ERK proteins. Selecting the appropriate assay format is critical to obtaining mechanistic insights, and assay conditions should be optimized for cell type, density, and culture format (monolayer, co-culture, or 3D systems).

Controls and Validation

Inclusion of proper experimental controls is essential. Negative controls without Motixafortide treatment allow baseline measurements of CXCR4 activity, while competitive binding or ligand-blocking controls help validate specificity. Replicates and independent experimental repeats are recommended to ensure statistical reliability.

Integration with Multi-Omic Studies

For mechanistic studies involving transcriptomics, proteomics, or metabolomics, Motixafortide can be integrated into multi-omic workflows to examine global changes in signaling networks. Computational modeling and pathway analysis can further enhance interpretation of the observed molecular effects.

Summary

Careful consideration of concentration, exposure duration, assay selection, and appropriate controls is essential for maximizing the utility of Motixafortide in in vitro research. Thoughtful experimental design ensures reproducible, high-quality data, enabling detailed mechanistic insights into CXCR4 receptor function, chemokine-mediated signaling, and cell migration processes.

Laboratory Safety & Handling Guidelines

Motixafortide is a high-purity research reagent intended for in vitro and molecular-level studies. Proper laboratory safety and handling procedures are essential to ensure safe use and to maintain compound integrity during experiments. Researchers should follow standard chemical and biological laboratory protocols when working with Motixafortide.

Personal Protective Equipment (PPE)

Always wear appropriate PPE, including lab coats, gloves, and safety goggles, when handling Motixafortide. Avoid direct contact with skin and eyes. In the event of accidental contact, immediately wash the affected area with plenty of water and seek medical advice if necessary.

Handling and Storage

Motixafortide should be handled in a clean, controlled laboratory environment, preferably within a chemical fume hood or biosafety cabinet to minimize exposure to airborne particles. The compound should be stored at −20 °C in a tightly sealed, moisture-free container, protected from light. Avoid repeated freeze-thaw cycles to maintain chemical stability.

Contamination and Waste Disposal

Prevent cross-contamination by using dedicated equipment and materials when preparing solutions or performing experiments. All waste containing Motixafortide must be collected in appropriate chemical waste containers and disposed of according to local regulations. Avoid release into the environment.

Emergency Measures

In case of accidental inhalation, move to fresh air immediately. For ingestion, rinse mouth thoroughly and seek medical attention. Laboratories should have appropriate spill kits and first aid supplies available and ensure all personnel are trained in emergency response procedures.

General Considerations

Motixafortide is strictly for research purposes and is not intended for human, veterinary, or clinical use. Follow institutional guidelines, national regulations, and chemical safety standards when handling this compound. Maintaining good laboratory practices, proper labeling, and secure storage ensures both researcher safety and experimental reproducibility.

Integration with Multi-Omic & Computational Studies

Motixafortide is ideally suited for integration into multi-omic and computational research workflows, enabling a comprehensive understanding of CXCR4-mediated signaling and cellular processes in vitro. Its selective CXCR4 antagonism provides a precise tool to dissect receptor-ligand interactions, intracellular pathways, and downstream molecular effects, making it highly compatible with omics-based experimental designs.

Proteomics Applications

In proteomic studies, Motixafortide can be used to investigate changes in protein expression, post-translational modifications, and signaling network alterations resulting from CXCR4 inhibition. High-resolution mass spectrometry or targeted proteomic approaches allow detailed mapping of pathway perturbations in response to receptor blockade.

Transcriptomics and Gene Expression Profiling

Motixafortide enables mechanistic studies at the transcriptional level by modulating CXCR4-dependent gene expression. RNA sequencing or qPCR analyses can reveal regulatory changes in chemokine-related pathways, migration-associated genes, and downstream effector molecules, providing insights into the broader molecular consequences of CXCR4 antagonism.

Computational Modeling and Pathway Analysis

Integration with computational approaches, such as molecular docking, receptor-ligand simulations, and pathway modeling, allows prediction and visualization of CXCR4-Motixafortide interactions. Computational analyses complement experimental data, enhancing understanding of receptor dynamics, binding affinities, and pathway crosstalk.

Multi-Omic Integration

By combining proteomic, transcriptomic, and metabolomic data, researchers can generate holistic models of CXCR4-mediated signaling networks. Motixafortide provides a reliable perturbation tool in these studies, enabling high-resolution mechanistic insights and identification of potential downstream targets or modulators within complex cellular systems.

Keywords

 CXCR4 antagonist, in vitro mechanism study, molecular mechanism analysis, high-purity research compound, China factory supply, bulk Motixafortide, wholesale research chemical

Shipping Guarantee

packaged and shipped with strict quality control to ensure the integrity and stability of the compound during transport. Each order is carefully labeled and sealed to prevent contamination or degradation. Shipments are trackable, allowing researchers to monitor delivery status in real time. Our logistics partners prioritize safe and timely delivery, minimizing the risk of delays. Special handling instructions can be accommodated for bulk or sensitive shipments. Overall, this ensures that Motixafortide arrives in optimal condition for immediate use in in vitro research applications.

Trade Assurance

Factory-direct supply from China guarantees authenticity, consistent high quality, and competitive pricing for Motixafortide. Bulk and wholesale orders are fully supported, making it feasible for long-term experimental projects and multi-lab collaborations. Trade assurance ensures that all transactions meet regulatory and contractual standards. Product batches undergo rigorous quality control to maintain reproducibility and research reliability. Researchers can request certification or batch-specific data as needed. This provides confidence in both product quality and supplier reliability for mechanistic studies.

Payment Support

We offer multiple flexible payment methods to accommodate global research institutions and laboratories. Accepted payment options include bank transfer (TT), major credit cards, and cryptocurrencies such as BTC, ETH, or USDT. Payments are processed securely to protect customer information and transaction integrity. Special arrangements can be made for bulk or recurring orders. Clear invoicing and documentation are provided for each transaction. This flexibility allows laboratories to manage budgets efficiently while accessing high-purity Motixafortide for their experiments.

Disclaimer

Motixafortide is strictly intended for research purposes in vitro and at the molecular level. It is not suitable for human, animal, or clinical applications. Researchers must adhere to all institutional, local, and national safety regulations when handling the compound. Proper laboratory safety protocols, including PPE and controlled handling, should always be followed. The manufacturer assumes no responsibility for misuse or applications outside approved research settings. Following these guidelines ensures safe, reliable, and reproducible experimental outcomes.

References

1. DrugBank – Motixafortide (DB14939)
   Comprehensive pharmacological profile, mechanism of action, and CXCR4 binding data.
   https://go.drugbank.com/drugs/DB14939

2. PubMed – Molecular Basis of Motixafortide-CXCR4 Interaction
   Structural and functional studies demonstrating CXCR4 antagonism and downstream signaling inhibition.
   https://pubmed.ncbi.nlm.nih.gov/36901829/

3. Drugs.com – Motixafortide Monograph
   Research-focused monograph with receptor pharmacology and in vitro study references.
   https://www.drugs.com/monograph/motixafortide.html

4. Synapse PatSnap – Motixafortide Mechanism Overview
   Analysis of molecular design, CXCR4 receptor binding, and in vitro research applications.
   https://synapse.patsnap.com/article/what-is-the-therapeutic-class-of-motixafortide

5. FDA Integrated Summary – Motixafortide Mechanistic Data
   Official regulatory documentation detailing CXCR4 inhibition and receptor occupancy.
   https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/217159Orig1s000IntegratedR.pdf