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| Targets |
Programmed cell death protein 1 (PD-1) and its ligand PD-L1. The PD-1/PD-L1 interaction is a key immune checkpoint that downregulates T cell activity, allowing cancer cells to evade the immune system. (D)-PPA 1 TFA is an antagonist that blocks this interaction, thereby reactivating the immune system's ability to attack tumor cells.
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| ln Vitro |
At 1.0 mg/mL, the interaction between PD-1/PD-L1 is blocked by (D)-PPA 1 TFA (0.2 mg/mL, 1.0 mg/mL) [1]. (d) -ppa 1 (3.125-100 μM; 24 h, 48 h) has no effect on CT26 cell proliferation and does not directly destroy tumor cells [1].
(D)-PPA 1 TFA binds directly to PD-1 with an affinity of 0.51 microM, effectively blocking the PD-1/PD-L1 interaction. In cell-based assays, it does not directly kill tumor cells or affect their growth. Instead, it functions by preventing the inhibition of T cells, thereby unleashing an anti-tumor immune response. It blocks the interaction between PD-1 and PD-L1 at a concentration of 1.0 mg/mL. |
| ln Vivo |
(D)-PPA 1 TFA (2 mg/kg; subcutaneous or intraperitoneal injection; once a day for 7 days) retards the development of mouse CT26 tumors [1]. Targeting tumor tissue in CT26 tumor-bearing mice, (D)-PPA 1 TFA (40 μg/mouse in 200 μL; iv; single dose) exhibits this property [1].
In vivo, (D)-PPA 1 TFA has shown significant anti-tumor efficacy. In a CT26 mouse colon carcinoma model, it is administered subcutaneously or intraperitoneally at a dose of 2 mg/kg once daily for 7 days, which inhibits tumor growth. Additionally, it has the ability to target tumor tissue, as demonstrated by the accumulation of the compound in the tumors of CT26-bearing mice after a single intravenous dose of 40 microg/mouse. |
| Enzyme Assay |
A surface plasmon resonance (SPR) assay is used to determine the binding affinity. Recombinant PD-1 protein is immobilized on a sensor chip. Various concentrations of (D)-PPA 1 TFA are flowed over the chip, and the resulting sensorgrams are analyzed to calculate the dissociation constant (KD), which is reported as 0.51 microM. This confirms the direct and high-affinity interaction between the peptide and its target.
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| Cell Assay |
A cell-based PD-1/PD-L1 blockade assay is used. In this system, PD-1-expressing effector cells and PD-L1-expressing target cells are co-cultured. When PD-1 engages PD-L1, a reporter signal is suppressed. The addition of (D)-PPA 1 TFA blocks this interaction, preventing the signal suppression, which allows for the measurement of peptide activity. The compound does not directly affect tumor cell growth, as shown by the lack of effect on CT26 cell viability.
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| Animal Protocol |
In vivo efficacy is evaluated in a CT26 syngeneic mouse colon carcinoma model. Mice are injected subcutaneously with CT26 tumor cells. Once the tumors are established, (D)-PPA 1 TFA is administered subcutaneously or intraperitoneally at a dose of 2 mg/kg once daily for 7 days. The anti-tumor effect is monitored by measuring tumor growth with calipers and comparing it to a vehicle-treated control group.
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| ADME/Pharmacokinetics |
As a D-peptide, (D)-PPA 1 TFA is designed to be resistant to hydrolysis by proteases, giving it a longer half-life in vivo compared to L-peptides. It is soluble in water at 100 mg/mL (59.89 mM). For in vivo administration, it can be formulated in saline or other physiologically compatible buffers. The D-amino acid configuration allows for effective targeting while maintaining metabolic stability.
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| Toxicity/Toxicokinetics |
No specific toxicity data is provided for (D)-PPA 1 TFA. In the CT26 mouse model, the compound was administered at 2 mg/kg for 7 days without reported adverse effects. D-peptides have low immunogenicity and are generally considered to be well-tolerated. Since the peptide works by modulating the immune system, there is a potential risk of immune-related adverse events at high doses.
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| References | |
| Additional Infomation |
(D)-PPA 1 TFA is a research-grade D-peptide used to study immune checkpoint inhibition for cancer therapy. Its D-amino acid composition makes it a potential therapeutic candidate with enhanced stability. This product is for research use only and is not FDA-approved for human use. A key reference is Chang HN, et al. Angew Chem Int Ed Engl. 2015;54(40):11760-4.
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| Molecular Formula |
C72H99F3N20O23
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| Molecular Weight |
1669.67
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| Related CAS # |
(D)-PPA 1;1620813-53-7
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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 (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 (~59.89 mM)
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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 | 0.5989 mL | 2.9946 mL | 5.9892 mL | |
| 5 mM | 0.1198 mL | 0.5989 mL | 1.1978 mL | |
| 10 mM | 0.0599 mL | 0.2995 mL | 0.5989 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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