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.
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- Pureté: 95.17%
- Formule: C189H282N42O55S.xC2HF3O2
- Masse moléculaire:4054.57 (free base)
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Stockage:
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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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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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Masse moléculaire 4054.57 (free base)
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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)
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
[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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