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| 1mg |
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| 10mg |
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| Targets |
ZY-1 targets vascular endothelial growth factor receptor-1 (VEGFR-1, also known as Flt-1). It co-localizes with membrane VEGFR-1 and effectively inhibits VEGF/PlGF-1-induced proliferation and tube formation of human umbilical vein endothelial cells (HUVECs). ZY-1 serves as a control molecule for ZY-2, a PKM2 fluorescent probe, and shows low fluorescence emission in HeLa cells, indicating minimal interference in imaging applications.
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| ln Vitro |
In vitro, ZY-1 effectively inhibits VEGF- and PlGF-1-induced proliferation of human umbilical vein endothelial cells (HUVECs) as measured by CCK-8 assay. It also inhibits tube formation of HUVECs on Matrigel. The peptide shows no significant effect on human corneal epithelial cell (HCEC) proliferation, indicating selectivity for endothelial cells. As a control molecule, ZY-1 shows low fluorescence emission in HeLa cells compared to ZY-2, making it suitable for background subtraction in imaging studies.
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| ln Vivo |
In vivo, topical administration of ZY-1 efficiently inhibits alkali-burn induced corneal neovascularization (NV) in a rat model. The anti-angiogenic effect is mediated through competitive binding to VEGFR-1. Importantly, long-term topical treatment with ZY-1 does not show any significant adverse effects on corneal and conjunctival functionality or morphology, as assessed by tear film break-up time (BUT) and histological examination. ZY-1 is a promising candidate for ocular anti-angiogenic therapy.
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| Enzyme Assay |
For in vitro angiogenesis assays, human umbilical vein endothelial cells (HUVECs) are seeded in 96-well plates and cultured in EGM-2 medium. For proliferation assay (CCK-8), cells are treated with ZY-1 (0.1-100 uM) in the presence of VEGF (10 ng/mL) or PlGF-1 (10 ng/mL) for 48 hours. CCK-8 reagent is added, and absorbance is measured at 450 nm.
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| Cell Assay |
For tube formation assay, Matrigel is polymerized in 96-well plates. HUVECs are pre-treated with ZY-1 (1-50 uM) for 30 minutes, then seeded on Matrigel with VEGF (10 ng/mL). After 6-8 hours at 37degC, tube formation is visualized under a microscope, and total tube length is quantified using ImageJ. For corneal epithelial cell assays, human corneal epithelial cells (HCECs) are treated similarly, and viability is assessed by CCK-8 to evaluate selectivity.
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| Animal Protocol |
For in vivo anti-angiogenic studies in a rat model of corneal neovascularization (NV), corneal NV is induced by alkali burn. Adult male Sprague-Dawley rats are anesthetized, and a circular filter paper (3 mm diameter) soaked in 1 N NaOH is applied to the central cornea for 40 seconds, followed by extensive washing with saline. ZY-1 is dissolved in sterile saline at concentrations of 0.1-1 mg/mL. Topical administration (5 uL, 4 times daily) is initiated immediately after injury and continued for 7-14 days. Corneal NV is evaluated daily under a slit-lamp microscope. At the end of the experiment, rats are euthanized, and corneas are excised for flat-mount preparation and stained with anti-CD31 antibody to quantify neovascular area. Corneal and conjunctival tissues are also collected for histological analysis (H&E staining). Tear film break-up time (BUT) is measured before sacrifice to assess ocular surface function. The safety profile is evaluated by comparing treated eyes with vehicle controls.
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| ADME/Pharmacokinetics |
As a peptide, ZY-1 is not expected to be orally bioavailable. Topical ocular administration is the primary route for anti-angiogenic studies. Detailed pharmacokinetic data (half-life, absorption, metabolism) are not available. The peptide should be stored as a lyophilized powder at -20degC and reconstituted in sterile saline or PBS before use. Solutions should be used fresh or stored at 4degC for short periods (up to 1 week).
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| Toxicity/Toxicokinetics |
In cell-based assays, ZY-1 shows no significant cytotoxicity toward human corneal epithelial cells (HCECs) at concentrations up to 100 uM, as measured by CCK-8 assay. In animal studies, long-term topical administration of ZY-1 (up to 14 days, 4 times daily) does not cause any detectable adverse effects on corneal and conjunctival morphology or function (tear film BUT). No signs of ocular irritation, inflammation, or systemic toxicity have been reported. Comprehensive toxicological studies have not been published.
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| References | |
| Additional Infomation |
ZY-1 is a research-grade peptide and is not approved for clinical use. It was derived from placental growth factor-1 (PlGF-1) and acts as a competitive VEGFR-1 antagonist. ZY-1 is also the control molecule for ZY-2, a fluorescent probe for PKM2 (pyruvate kinase M2). The sequence of ZY-1 is not provided in the public literature. The peptide is typically stored at -20degC as a lyophilized powder, protected from light and moisture.
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| Molecular Formula |
C23H26F3N3O4
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| Molecular Weight |
465.47
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| Appearance |
Yellow to orange 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1484 mL | 10.7418 mL | 21.4837 mL | |
| 5 mM | 0.4297 mL | 2.1484 mL | 4.2967 mL | |
| 10 mM | 0.2148 mL | 1.0742 mL | 2.1484 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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