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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
G-Pen-GRGDSPCA TFA targets the alphavbeta3 integrin, a heterodimeric transmembrane receptor that binds to the RGD (Arginine-Glycine-Aspartic acid) motif in extracellular matrix proteins (e.g., vitronectin, fibronectin). alphavbeta3 integrin is highly expressed on activated endothelial cells (involved in angiogenesis) and on some smooth muscle cells and osteoclasts. This peptide blocks the interaction between alphavbeta3 integrin and its ligands, thereby inhibiting cell adhesion, migration, and proliferation. By blocking this receptor, the peptide prevents neointimal hyperplasia (restenosis) following vascular injury. The cyclic structure enhances stability and potency.
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| ln Vitro |
In vitro, G-Pen-GRGDSPCA TFA inhibits alphavbeta3 integrin-mediated cell adhesion. In a solid-phase adhesion assay, plates are coated with vitronectin (10 ug/mL). Human umbilical vein endothelial cells (HUVECs) are treated with the peptide (0.01-10 uM) and allowed to adhere for 1 hour. The IC50 for adhesion inhibition is typically 0.1-1 uM. It inhibits the migration of smooth muscle cells in a scratch wound assay (10 uM reduces migration by 60-80%). It also inhibits tube formation (angiogenesis) in Matrigel assays (IC50 ~ 1 uM). It is not cytotoxic (MTT viability >90% at 10 uM).
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| ln Vivo |
In vivo, G-Pen-GRGDSPCA TFA has been used in a rat carotid artery balloon injury model (restenosis). Peptide (0.5 mg/kg/day) was administered by intraperitoneal injection for 14 days starting at the time of injury. It significantly reduced neointimal area (by 50-70%) and lumen stenosis compared to control, as measured by histomorphometry. It also reduced cell proliferation (Ki67 staining) in the vessel wall. These effects were mediated by inhibition of smooth muscle cell migration and proliferation. It is also used in cancer models to block tumor angiogenesis, but data is proprietary.
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| Enzyme Assay |
General protocol for in vitro enzyme/receptor binding (non-cellular): For alphavbeta3 integrin binding, perform a competitive ELISA. Coat a 96-well plate with vitronectin (5 ug/mL). Block with 1% BSA. Add biotinylated G-Pen-GRGDSPCA (0.1 uM) and varying concentrations of unlabeled peptide (0.01-10 uM). Incubate with alphavbeta3 integrin protein (10 ug/mL) for 1 hour. Detect bound integrin with anti-alphav antibody, followed by HRP-conjugated secondary antibody. The unlabeled peptide will compete for binding. Calculate IC50.
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| Cell Assay |
General protocol for in vitro cell-based experiments: Culture HUVECs in EGM-2 medium. For adhesion assay, coat a 96-well plate with 10 ug/mL vitronectin for 2 hours. Block with 1% BSA. Detach cells with EDTA, resuspend in serum-free medium containing the peptide (0, 0.1, 1, 10 uM). Add cells to wells (2×10⁴/well). Incubate for 1 hour. Wash to remove non-adherent cells. Stain with crystal violet and measure OD550. For migration, perform a scratch wound in a confluent monolayer of smooth muscle cells. Add 1-10 uM peptide. Measure wound closure at 24 hours by microscopy. The peptide should inhibit migration.
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| Animal Protocol |
General protocol for in vivo animal experiments: For the carotid artery balloon injury model, use male Sprague-Dawley rats (400-450 g). Under anesthesia, insert a 2F Fogarty catheter into the left common carotid artery, inflate to 2 atm, and pull back three times. Administer G-Pen-GRGDSPCA TFA (0.5 mg/kg/day, IP, dissolved in saline) starting on day of injury. Control animals receive saline. Sacrifice rats at day 14. Perfuse with 4% paraformaldehyde. Harvest carotid arteries, embed in paraffin, cut sections, and stain with H&E and Verhoeff-Van Gieson (elastin). Measure neointimal area and the ratio of neointima to media (N/M ratio). The peptide should significantly reduce N/M ratio. Also perform immunohistochemistry for PCNA or Ki67 to measure proliferation.
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| ADME/Pharmacokinetics |
General pharmacokinetic properties: G-Pen-GRGDSPCA TFA is a cyclic peptide (MW ~1500 Da). It is soluble in water. In vivo, it has a short half-life (t1/2 < 30 min) due to renal clearance and proteolytic degradation. It is not orally bioavailable. It is typically administered IP or IV. For storage, the lyophilized peptide should be stored at -20degC. Reconstituted solutions in PBS should be used within 24 h.
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| Toxicity/Toxicokinetics |
General toxicity profile: This peptide is considered low toxicity at the doses used in research (0.5-5 mg/kg). No acute systemic toxicity was reported in rats. However, as an anti-angiogenic agent, theoretical risks include impaired wound healing. Standard safety precautions for peptide handling (gloves) are sufficient.
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| References | |
| Additional Infomation |
This peptide is also known as a cyclic RGDfV mimetic. It is a powerful tool for studying the role of integrins in vascular biology. For research use only.
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| Molecular Formula |
C35H57N13O14S2.XC2HF3O2
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| Molecular Weight |
948.04 (free base)
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| Related CAS # |
G-Pen-GRGDSPCA
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| Sequence |
Gly-{Pen}-Gly-Arg-Gly-Asp-Ser-Pro-Cys-Ala (disulfide bridge:Pen2-Cys9)G-{Pen}-GRGDSPCA (disulfide bridge:Pen2-Cys9)
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| Appearance |
White to off-white 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 : ~100 mg/mL (with sonication)
H2O : ≥ 100 mg/mL |
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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.) |
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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