| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
PSMA targeting peptide TFA targets prostate-specific membrane antigen (PSMA), a type II transmembrane glycoprotein that is highly expressed on the surface of prostate cancer cells. PSMA is also known as folate hydrolase 1 (FOLH1) and glutamate carboxypeptidase II (GCPII). It is involved in folate metabolism and has been exploited as a target for prostate cancer imaging and therapy due to its restricted expression in normal tissues and high expression in prostate cancer. The peptide sequence GRFLTGGTGRLLRIS is designed to bind specifically to PSMA. By targeting PSMA, the peptide enables the delivery of therapeutic payloads, such as siRNAs, specifically to prostate cancer cells.
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| ln Vitro |
In vitro, PSMA targeting peptide TFA binds specifically to PSMA-expressing prostate cancer cells. The peptide can be used for targeted delivery of glucose-regulated protein (GRP)-silencing siRNAs in prostate cancer cells. By delivering siRNAs that silence GRP, the peptide enables the study of GRP function in prostate cancer and the potential therapeutic effects of GRP silencing. The peptide's binding specificity for PSMA can be assessed in cell-based assays using PSMA-positive and PSMA-negative cell lines. The TFA salt form enhances solubility for formulation purposes. However, specific quantitative data such as binding affinity (Kd) or IC50 values have not been extensively reported in the available literature.
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| ln Vivo |
In vivo activity of PSMA targeting peptide TFA has not been extensively reported in the available literature. Based on its ability to target PSMA and deliver siRNAs to prostate cancer cells in vitro, the peptide would be expected to have potential for in vivo applications in prostate cancer imaging and therapy. However, specific animal model studies, dosing regimens, and quantitative outcomes have not been reported. The peptide's small size and targeting specificity suggest that it may have favorable biodistribution and tumor penetration properties. Further in vivo studies would be required to characterize its efficacy, safety, and pharmacokinetic properties in animal models of prostate cancer.
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| Enzyme Assay |
In vitro binding assay protocols for PSMA targeting peptide TFA typically involve assessing its binding affinity for PSMA. A standard protocol would involve using PSMA-positive prostate cancer cells (e.g., LNCaP cells) and PSMA-negative cells (e.g., PC-3 cells) as controls. Cells are incubated with fluorescently labeled or radiolabeled PSMA targeting peptide TFA at varying concentrations, and binding is assessed by flow cytometry, fluorescence microscopy, or scintillation counting. Competition binding assays can be performed using unlabeled peptide to determine specificity. For siRNA delivery studies, cells are treated with the peptide-siRNA complex, and siRNA uptake and target gene knockdown (e.g., GRP silencing) are assessed by qPCR or Western blot. Appropriate controls include cells treated with siRNA alone or with a non-targeting peptide.
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| Cell Assay |
In vitro cell-based assay protocols for PSMA targeting peptide TFA typically involve assessing its ability to deliver siRNAs to prostate cancer cells. A standard protocol would involve seeding PSMA-positive prostate cancer cells (e.g., LNCaP cells) in multi-well plates. The peptide is complexed with GRP-targeting siRNAs (or control siRNAs) and added to the cells. After incubation for 24-72 hours, cells are harvested, and GRP mRNA and protein levels are assessed by qPCR and Western blot, respectively. Cell viability and proliferation can be assessed using MTT or CellTiter-Glo assays to evaluate the functional effects of GRP silencing. For binding studies, cells are incubated with fluorescently labeled peptide, and binding is assessed by flow cytometry or fluorescence microscopy. Appropriate controls include cells treated with siRNA alone, non-targeting peptide, or vehicle.
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| Animal Protocol |
In vivo animal experimental protocols for PSMA targeting peptide TFA have not been reported in the available literature. Based on its ability to target PSMA and deliver siRNAs to prostate cancer cells in vitro, potential studies might involve using mouse xenograft models of prostate cancer. A hypothetical protocol would involve implanting PSMA-positive prostate cancer cells (e.g., LNCaP cells) subcutaneously in immunodeficient mice, allowing tumors to reach a certain size, and then administering the peptide-siRNA complex via intravenous injection. Treatment would typically be administered multiple times over 2-4 weeks. Endpoints would include tumor volume measurement, tumor weight at necropsy, assessment of GRP knockdown in tumor tissues by qPCR and Western blot, and evaluation of therapeutic efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of PSMA targeting peptide TFA have not been characterized in published studies. As a peptide, the compound would be expected to have limited oral bioavailability due to susceptibility to proteolytic degradation. Following parenteral administration, it would likely be cleared through proteolysis and renal excretion. The TFA salt form enhances solubility for formulation purposes. Specific PK parameters such as half-life, Cmax, AUC, bioavailability, volume of distribution, and clearance have not been reported. The compound's stability in biological matrices and its metabolic fate remain uncharacterized. Further pharmacokinetic studies would be required to understand its absorption, distribution, metabolism, and excretion profile.
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| References | |
| Additional Infomation |
PSMA targeting peptide TFA (PSMA-1 TFA) is a research-grade peptide that targets prostate-specific membrane antigen (PSMA). It has the sequence GRFLTGGTGRLLRIS and can be used for targeted delivery of GRP-silencing siRNAs in prostate cancer cells. The compound has not entered clinical trials and is not approved for any therapeutic indication. Its mechanism of action involves specific binding to PSMA on prostate cancer cells, enabling the targeted delivery of therapeutic payloads. The compound is available exclusively for research purposes and is not intended for diagnostic, therapeutic, or human applications.
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| Molecular Formula |
C70H122N24O19.XC2HF3O2
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| Molecular Weight |
1603.87 (free base)
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| Appearance |
Typically exists as solid at room temperature
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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) |
H2O :~100 mg/mL (with sonication)
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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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