pH-Low Insertion Peptide
Based on 1 Customer Validation
pH-Low Insertion Peptide (pHLIP) is a short, pH-responsive peptide capable of inserting across a cell membrane to form a transmembrane helix at acidic pH. pH-Low Insertion Peptide targets the acidic tumor microenvironment for tumors at early and metastatic stages with high specificity, used as a specific ligand. pH-Low Insertion Peptide successfully modify polylysine polymers to have the pH-responsive capability. pH-Low Insertion Peptide-based targeting of cancer presents an opportunity to monitor metabolic changes, and to selectively deliver imaging and therapeutic agents to tumors.
For research use only. We do not sell to patients.
- Purity: 99.38%
- CAS No.: 2293160-09-3
- Formula: C189H28N4O55S
- Molecular Weight:4054.56
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Storage:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
pH-Low Insertion Peptide (5 μM, 2 h) combined with peptide nucleic acid (peptide nucleic acid, PNA) significantly increases PNA delivery at pH 6.2 in A549 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:5 μM
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Incubation Time:2 h
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Result:Significantly increases PNA delivery combined with PNA at pH 6.2 in A549 cells.
pH-Low Insertion Peptide (10 μM, i.v., a single dose for 24 h) can clearly differentiate between regions of primarily tumor cells and nonmalignant stromal tissues, also accumulates the hypoxia marker Pimonidazole (HY-105129A) and relates to the production of acidic glucose metabolites in MMTV-Py MT mice[2].
pH-Low Insertion Peptide (0.2 μmol/kg, i.v., a single dose for 24 h) demonstrats excellent tumor targeting combined with PNA in mice seeded melanoma tumors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Murine 4T1 xenograft model[2]
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Dosage:50 μM
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Administration:a single tail vein injection, tumors collected at 4, 24, and 48 h after administration
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Result:The spatial distribution and the intensity profiles of all pHLIPs in tumors were identical in murine 4T1 xenograft mode.
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Animal Model:FVB/N-Tg(MMTV-PyVT)634Mul/J transgenic female mice developed palpable mammary tumors at 12-15 weeks of age[2]
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Dosage:10 μM
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Administration:i.v., a single dose for 24 h
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Result:Clearly differentiated between regions of primarily tumor cells and nonmalignant stromal tissues.
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Animal Model:6-week old C57BL/6 mice seeded melanoma tumors[3]
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Dosage:0.2 μmol/kg
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Administration:intravenously injected via the retro-orbital sinus, a single dose for 24 h
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Result:All the pH-Low Insertion Peptide-PNAs demonstrated excellent tumor targeting.
Chemical Information
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CAS No. 2293160-09-3
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Appearance Solid
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Molecular Weight 4054.56
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Formula C189H28N4O55S
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Color White to off-white
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Synonyms
pHLIP
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Sequence
Ala-Cys-Glu-Gln-Asn-Pro-Ile-Tyr-Trp-Ala-Arg-Tyr-Ala-Asp-Trp-Leu-Phe-Thr-Thr-Pro-Leu-Leu-Leu-Leu-Asp-Leu-Ala-Leu-Leu-Val-Asp-Ala-Asp-Glu-Thr
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Sequence Shortening
ACEQNPIYWARYADWLFTTPLLLLDLALLVDADET
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 100 mg/mL (24.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (0.62 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (287 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Yushuang Wei, et al. pH-responsive pHLIP (pH low insertion peptide) nanoclusters of superparamagnetic iron oxide nanoparticles as a tumor-selective MRI contrast agent. Acta Biomater. 2017 Jun;55:194-203. [Content Brief]
[2]. Adochite RC, et al. Targeting breast tumors with pH (low) insertion peptides[J]. Mol Pharm. 2014 Aug 4;11(8):2896-905. [Content Brief]
[3]. Svoronos AA, et al. Tumor-Targeted, Cytoplasmic Delivery of Large, Polar Molecules Using a pH-Low Insertion Peptide[J]. Mol Pharm. 2020 Feb 3;17(2):461-471. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.2466 mL | 1.2332 mL | 2.4664 mL | 6.1659 mL |
| 5 mM | 0.0493 mL | 0.2466 mL | 0.4933 mL | 1.2332 mL | |
| 10 mM | 0.0247 mL | 0.1233 mL | 0.2466 mL | 0.6166 mL | |
| 15 mM | 0.0164 mL | 0.0822 mL | 0.1644 mL | 0.4111 mL | |
| 20 mM | 0.0123 mL | 0.0617 mL | 0.1233 mL | 0.3083 mL |
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