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  6. pH-Low Insertion Peptide

pH-Low Insertion Peptide  (Synonyms: pHLIP)

Cat. No.: HY-P4116 Purity: 96.37%
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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.

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pH-Low Insertion Peptide Chemical Structure

pH-Low Insertion Peptide Chemical Structure

CAS No. : 2293160-09-3

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5 mg USD 320 In-stock
10 mg USD 520 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of pH-Low Insertion Peptide:

pH-Low Insertion Peptide Related Antibodies

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Description

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[1][2][3].

In Vitro

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.

pH-Low Insertion Peptide Related Antibodies

Immunofluorescence[3]

Cell Line: A549 cells
Concentration: 5 μM
Incubation Time: 2 h
Result: Significantly increases PNA delivery combined with PNA at pH 6.2 in A549 cells.
In Vivo

pH-Low Insertion Peptide (50 μM, a single tail vein injection, 4, 24, and 48 h) variants shows the pH-dependent tumor targeting and different blood clearance profiles, the overall tumor spatial distributions are identical in murine 4T1 xenograft mode[2].
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.

Animal Model: Murine 4T1 xenograft model[2]
Dosage: 50 μM
Administration: a single tail vein injection, tumors collected at 4, 24, and 48 h after administration
Result: The spatial distribution and the intensity profiles of all pHLIPs in tumors were identical in murine 4T1 xenograft mode.
Animal Model: FVB/N-Tg(MMTV-PyVT)634Mul/J transgenic female mice developed palpable mammary tumors at 12-15 weeks of age[2]
Dosage: 10 μM
Administration: i.v., a single dose for 24 h
Result: Clearly differentiated between regions of primarily tumor cells and nonmalignant stromal tissues.
Animal Model: 6-week old C57BL/6 mice seeded melanoma tumors[3]
Dosage: 0.2 μmol/kg
Administration: intravenously injected via the retro-orbital sinus, a single dose for 24 h
Result: All the pH-Low Insertion Peptide-PNAs demonstrated excellent tumor targeting.
Molecular Weight

4054.56

Formula

C189H28N4O55S
CAS No.
Appearance

Solid

Color

White to off-white

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
Sequence Shortening

ACEQNPIYWARYADWLFTTPLLLLDLALLVDADET
Shipping

Room temperature in continental US; may vary elsewhere.
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.2466 mL 1.2332 mL 2.4664 mL
5 mM 0.0493 mL 0.2466 mL 0.4933 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (0.62 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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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pH-Low Insertion Peptide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

pH-Low Insertion Peptide2293160-09-3pHLIPOtherspH-responsive peptideacidic tumor microenvironmentspecific ligandcancerdeliverInhibitorinhibitorinhibit

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