| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Human PD-L1 inhibitor V TFA targets the PD-1 protein on the surface of T cells. By binding to PD-1, the peptide blocks the interaction with PD-L1, which is often overexpressed on tumor cells and antigen-presenting cells. Inhibition of the PD-1/PD-L1 axis restores T cell activation, proliferation, and cytotoxic activity against cancer cells. The peptide is designed with anchor residues Y56, R113, A121, D122, and Y123.
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| ln Vitro |
The peptide known as human PD-L1 inhibitor V(Ar5M_2) has the anchor residues Y56, R113, A121, D122, and Y123 in its design[1].
The binding affinity of Human PD-L1 inhibitor V TFA to human PD-1 is evaluated using a cell-free surface plasmon resonance (SPR) assay or biolayer interferometry (BLI). The peptide is immobilized on a sensor chip or plate, and recombinant PD-1 protein is flowed over the surface at varying concentrations. The Kd value is determined to be 3.32 microM. The peptide also inhibits PD-1/PD-L1 binding in competition ELISA assays. |
| ln Vivo |
In cellular assays, the inhibitory activity of Human PD-L1 inhibitor V TFA is assessed in a co-culture system of PD-L1-expressing tumor cells and PD-1-expressing T cells. The peptide is added at varying concentrations (0.1-100 microM), and T cell activation is measured by IL-2 production (ELISA), IFN-gamma secretion, and T cell proliferation (CFSE dilution). Increased T cell activity in the presence of the peptide indicates successful blockade of the PD-1/PD-L1 interaction.
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| Enzyme Assay |
The PD-1/PD-L1 binding inhibition assay is performed using a competitive ELISA. Recombinant human PD-1 protein is coated onto a 96-well plate. Biotinylated PD-L1 is incubated with varying concentrations of Human PD-L1 inhibitor V TFA (0.1-100 microM) before being added to the plate. Bound PD-L1 is detected using streptavidin-HRP and a colorimetric substrate. The concentration required to inhibit 50% of binding (IC50) is calculated from the dose-response curve. The Kd for PD-1 binding is determined by SPR.
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| Cell Assay |
A Jurkat T cell line expressing PD-1 is co-cultured with PD-L1-expressing CHO cells (CHO-PD-L1). The test peptide (Human PD-L1 inhibitor V TFA) is added at concentrations ranging from 0.1 to 100 microM. After 24-48 hours, the supernatant is collected for IL-2 and IFN-gamma measurement by ELISA. T cell activation is also assessed by flow cytometry for CD69 expression. The peptide concentration that restores half-maximal T cell activation is determined.
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| Animal Protocol |
Human PD-L1 inhibitor V TFA can be evaluated in a mouse model bearing PD-L1-expressing tumor xenografts (e.g., MC38 colon carcinoma or B16 melanoma) in humanized PD-1/PD-L1 mice. The peptide is administered intraperitoneally (10-50 mg/kg) daily for 10-14 days. Tumor volume is measured by caliper, and tumor-infiltrating lymphocytes are analyzed by flow cytometry for CD8+ T cell activation markers (IFN-gamma, granzyme B). The peptide's anti-tumor efficacy is compared to anti-PD-1 antibody therapy.
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| ADME/Pharmacokinetics |
Human PD-L1 inhibitor V TFA is a peptide with a molecular weight of approximately 2.5-3 kDa (estimated). It is formulated in aqueous buffers (e.g., PBS) for in vitro and in vivo use. The TFA salt enhances solubility and stability. Peptides generally have short half-lives in vivo due to rapid proteolytic degradation; thus, multiple daily injections or a continuous infusion (e.g., via osmotic pump) may be required for sustained activity. PEGylation or other modifications could improve pharmacokinetic properties.
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| Toxicity/Toxicokinetics |
Human PD-L1 inhibitor V TFA is a research-grade peptide and has not undergone formal toxicology studies. It is expected to have low toxicity based on its mechanism of action (blocking an immune checkpoint) and its peptide nature. However, at high doses, non-specific immune activation or immunogenicity could occur. Standard laboratory safety precautions (gloves, lab coat, safety glasses) should be followed when handling the compound.
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| References | |
| Additional Infomation |
Human PD-L1 inhibitor V TFA is a research compound intended for studying the PD-1/PD-L1 immune checkpoint pathway and for developing peptide-based cancer immunotherapies. It is derived from the peptide Ar5M_2 and has a sequence containing anchor residues Y56, R113, A121, D122, and Y123. This product is for research use only and is not approved for clinical use. It offers an alternative to antibody-based PD-1/PD-L1 blockade for research applications.
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| Molecular Formula |
C65H104N20O18S.XC2HF3O2
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| Molecular Weight |
1485.71 (free base)
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| Related CAS # |
Human PD-L1 inhibitor V;2815311-61-4
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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) |
H2O :~100 mg/mL
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (Infinity mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(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.
Products are for research use only; We do not sell to patients
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