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| Targets |
Cypate hydrochloride does not bind to a specific molecular target; its function is based on its physicochemical optical properties. As a fluorescent dye, it passively accumulates in tumor tissues via the enhanced permeability and retention (EPR) effect. Upon excitation with NIR light (typically 720-780 nm), it emits fluorescence (800-820 nm), enabling deep tissue imaging. When used as a photosensitizer, it generates reactive oxygen species (ROS) and heat upon NIR irradiation.
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| ln Vitro |
According to the study, Cypate coupled upconversion nanoparticles (UCNP-cy) loaded with anti-heat shock protein 70 small interfering RNA genes (UCNP-cy-siRNA) can cause targeted cellular damage and have anti-tumor properties [1]. In order to track, label, and photograph particular biomolecules or cells, Cypate can also be connected to CBT (Cysteine-containing Peptide Backbone Tag). For instance, cathepsin B (CTSB) activity can be specifically seen and tracked in real time in tumors and cells that overexpress CTSB using Cypate-CBT, a near-infrared photoacoustic (PA) probe. Cypate-CBT increases the strength and duration of the PA signal at the tumor site by entering CTSB-overexpressing cells, where it is then subjected to glutathione reduction and CTSB cleavage to produce cypate nanoparticles, or Cypate-CBT-NPs. For the clinical diagnosis of early cancer, cipate-CBT has the potential to be a useful PA imaging agent [2].
Cypate has high photostability and optical properties, allowing for long-term imaging without significant photobleaching. In aqueous solutions, its fluorescence quantum yield is moderate (approx. 5-10%), but it is significantly enhanced when loaded into liposomes or nanoparticles via pi-pi stacking aggregation. Liposomal encapsulation increases singlet oxygen quantum yield and photothermal conversion efficiency. Cypate is non-toxic up to 50 microM in most cell lines. |
| ln Vivo |
Cypate is a near-infrared fluorescent dye that exhibits high photostability and optical properties, making it a common choice for near-infrared optical imaging, optical development, tumor labeling, and drug delivery in vivo. In tumor-bearing mouse models, intravenous administration of Cypate or Cypate-nanoparticle conjugates enables real-time fluorescence imaging of tumor margins with high signal-to-background ratio. Upon NIR laser irradiation (808 nm, 0.5-1.5 W/cm2), effective photothermal ablation of tumors is achieved, as demonstrated by temperature rises (deltaT=20-35degC) and tumor growth inhibition.
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| Enzyme Assay |
The NIR absorption and fluorescence emission spectra are measured in phosphate-buffered saline (PBS, pH 7.4, 1% DMSO) or ethanol. A stock solution of Cypate is prepared at 1 mg/mL. The absorption spectrum is recorded from 400-900 nm using a UV-Vis-NIR spectrophotometer; absorption maximum is typically 730-770 nm. The fluorescence emission spectrum is measured using a spectrofluorophotometer with excitation at the absorption maximum; emission maximum is approximately 780-810 nm. Fluorescence quantum yield is determined using indocyanine green (Φ=0.14 in DMSO) as a reference standard. Photostability is assessed by continuous irradiation with a xenon lamp for 60 minutes and monitoring the decrease in fluorescence intensity.
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| Cell Assay |
Standard cellular uptake and imaging experiments: cells (e.g., 4T1 murine breast cancer or HeLa cells) are seeded in glass-bottom dishes (1 × 10⁵ cells/dish) and cultured for 24 hours. Cypate hydrochloride (1-20 microM) in serum-free medium is added, and cells are incubated for 1-6 hours at 37degC. After three washes with PBS, cells are fixed with 4% paraformaldehyde for 15 minutes. Confocal laser scanning microscopy is performed using a 635 nm excitation laser and 650-750 nm long-pass or band-pass emission filter. For viability assays (MTT or CCK-8), cells are treated with Cypate (0-100 microM) for 24-48 hours, then exposed to NIR laser (808 nm, 1 W/cm2, 5 min) to assess photothermal cytotoxicity.
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| Animal Protocol |
For in vivo tumor imaging, female BALB/c nude mice bearing subcutaneous 4T1 tumors (approx. 150 mm3) are used. Cypate (1-5 mg/kg body weight) or Cypate-labeled nanoparticles (e.g., Cypate encapsulated in liposomes or conjugated to targeting ligands) are administered intravenously via tail vein injection (200 microL volume). At various time points (1, 4, 8, 12, 24, 48 hours), mice are anesthetized with isoflurane. Whole-body fluorescence images are acquired using an in vivo imaging system (excitation: 710-760 nm, emission: 810-880 nm, exposure time: 100-500 ms). For photothermal therapy, the tumor region of Cypate-injected mice is irradiated with an 808 nm NIR laser at 1-1.5 W/cm2 for 5-10 minutes. Tumor volume and surface temperature (by infrared thermal camera) are monitored every 2-3 days.
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| ADME/Pharmacokinetics |
Cypate is a small molecule dye (approx. MW = 800 g/mol). After intravenous injection, it has a relatively short circulation half-life (approx. 10-30 min in mice) due to rapid renal clearance unless encapsulated in nanoparticles or conjugated to a carrier such as albumin or polymer. The primary route of elimination is renal/fecal excretion. The molecule does not undergo significant metabolic transformation. Liposomal encapsulation dramatically increases plasma half-life to several hours and enhances tumor accumulation via the EPR effect. In photodynamic/photothermal applications, the compound is activated on-site by NIR light at the target tissue.
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| Toxicity/Toxicokinetics |
Cypate hydrochloride has a favorable safety profile with low intrinsic cytotoxicity. No significant acute toxicity is observed at doses up to 50 mg/kg in mice (intravenous, single dose). Hematology and serum biochemistry markers remain within normal ranges. No phototoxicity is observed without NIR light activation. The compound does not cause significant weight loss or clinical signs of distress in animals at therapeutic imaging or photothermal ablation doses (0.5-5 mg/kg). However, NIR laser irradiation of Cypate-containing tumors can cause moderate thermal injury to surrounding normal tissue if laser parameters (power density, duration) are not carefully optimized.
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| References |
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| Additional Infomation |
Cypate is a near-infrared fluorescent dye that belongs to the family of photosensitizers. It has high photostability and optical properties, and is often used in near-infrared optical imaging, as well as optical development, tumor marking, and drug delivery. Additionally, Cypate is used as a molecular probe with targeting molecules (such as CBT or small interfering RNA) to achieve highly efficient detection and imaging of specific cells or tissues. The molecule exhibits enhanced photothermal conversion and singlet oxygen generation when incorporated into liposomes due to pi-pi aggregation. Cypate hydrochloride is strictly for research use and not approved for clinical diagnostic or therapeutic use.
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| Molecular Formula |
C41H41CLN2O4
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| Molecular Weight |
661.23
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| Related CAS # |
Cypate;95837-47-1
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| Appearance |
Green to dark green solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~12.5 mg/mL (~18.90 mM)
H2O :< 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (1.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.25 mg/mL (1.89 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5123 mL | 7.5617 mL | 15.1233 mL | |
| 5 mM | 0.3025 mL | 1.5123 mL | 3.0247 mL | |
| 10 mM | 0.1512 mL | 0.7562 mL | 1.5123 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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