pH-Low Insertion Peptide TFA
Based on 1 Customer Validation
pH-Low Insertion Peptide TFA (pHLIP TFA) 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 TFA targets the acidic tumor microenvironment for tumors at early and metastatic stages with high specificity, used as a specific ligand. pH-Low Insertion Peptide TFA successfully modifys polylysine polymers to have the pH-responsive capability. pH-Low Insertion Peptide TFA -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: 95.17%
- Formula: C189H282N42O55S.xC2HF3O2
- Molecular Weight:4054.57 (free base)
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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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
pH-Low Insertion Peptide TFA (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 TFA (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 TFA (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 pHLIP TFAs 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 TFA-PNAs demonstrated excellent tumor targeting.
Chemical Information
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Appearance Solid
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Molecular Weight 4054.57 (free base)
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Formula C189H282N42O55S.xC2HF3O2
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Color White to off-white
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Synonyms
pHLIP TFA
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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)
Purity & Documentation
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Data Sheet (284 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 TFA [J]. Mol Pharm. 2020 Feb 3;17(2):461-471. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
pH-Low Insertion Peptide TFA Related Classifications
HY-P4116A Related Classifications
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