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HO-PEG-CH2COOH (MW 10000)

Cat No.:V76920 Purity: ≥98%
HO-PEG-CH2COOH (MW 10000) is a PEG polymer with -COOH that can be used as a PROTAC (PROteolysis TArgeting Chimera) linker to prepare PROTACs.
HO-PEG-CH2COOH (MW 10000)
HO-PEG-CH2COOH (MW 10000) Chemical Structure Product category: PROTAC Linkers
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
Other Sizes
Official Supplier of:
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Product Description
HO-PEG-CH2COOH (MW 10000) is a PEG polymer with -COOH that can be used as a PROTAC (PROteolysis TArgeting Chimera) linker to prepare PROTACs.
HO-PEG-CH2COOH (MW 10000) is a heterobifunctional polyethylene glycol (PEG) derivative with a hydroxyl group (-OH) and a carboxylic acid group (-CH2COOH). The molecular weight is 10,000 Da, which is smaller than the 35 kDa version but still above the renal clearance threshold for PEG in rodents (≈30-50 kDa). This PEG is used as a linker for bioconjugation, drug delivery, and surface modification. The carboxylic acid can be activated (e.g., with EDC/NHS) to conjugate to amine-containing molecules (proteins, peptides, small molecules), while the hydroxyl group provides an inert or further modifiable end. It is a research reagent, not a drug.
Biological Activity I Assay Protocols (From Reference)
Targets
No specific biological target. HO-PEG-CH2COOH (MW 10000) is a synthetic polymer, not a pharmacologically active compound. It does not bind to receptors or enzymes. Its primary use is as a PEGylation reagent to modify drugs, proteins, or nanoparticles. PEGylation imparts benefits such as increased solubility, reduced immunogenicity, extended circulation half-life, and decreased proteolysis. The 10 kDa size is commonly used for conjugation to small molecules or peptides where a moderate increase in molecular weight is desired. The PEG spacer provides flexibility and hydrophilicity. The carboxylic acid end allows site-specific conjugation. The hydroxyl end can be capped or used for further chemistry. This product is a tool for drug delivery research.
ln Vitro
Not applicable. HO-PEG-CH2COOH (MW 10000) itself has no direct biological activity. It is not used in in vitro assays to inhibit enzymes or affect cell function. At typical concentrations used in conjugation (0.1-10 mg/mL), it is non-toxic and does not interfere with cell growth or signaling. Its purpose is to be coupled to active molecules. After conjugation, the PEG moiety may alter the activity (e.g., reduce potency due to steric hindrance) but enhance pharmacokinetics. As a reagent, it is not evaluated for in vitro efficacy.
ln Vivo
Not applicable. The polymer is not administered alone in vivo. When conjugated to a drug or protein, the conjugate can be dosed. For example, a PEG10k-cytokine conjugate may show improved half-life and reduced immunogenicity. In preclinical studies, high molecular weight PEGs (10 kDa) have a plasma half-life of several hours to days in mice (dependent on species and dose). They are generally well-tolerated but may cause vacuolation in renal tubules at high doses. The compound is for research use as a linker; it is not a therapeutic.
Enzyme Assay
For quality control, the PEG can be characterized by GPC (gel permeation chromatography) to confirm molecular weight and polydispersity. Carboxylic acid content can be quantified by titration or by a colorimetric assay (e.g., using Toluidine Blue O). Activation to NHS ester is typically verified by reaction with a small amine (e.g., ethylamine) and detection of the amide by FTIR or HPLC. For conjugation to a model protein (e.g., lysozyme or BSA), dissolve PEG-COOH (10 kDa) in MES buffer (pH 5.5) with EDC (5-10 eq) and NHS (5-10 eq), activate for 15-30 min. Add the protein in PBS (pH 7.4) at a molar ratio of 1:1 to 1:10 (protein:PEG). Incubate 2-4 h. Purify by dialysis or ultrafiltration. Analyze conjugation efficiency by SDS-PAGE or MALDI-TOF. No direct receptor binding assay is performed.
Cell Assay
Not applicable. HO-PEG-CH2COOH (MW 10000) is not used directly in cell-based assays. It can be used to PEGylate cell surfaces or to prepare PEG-coated nanoparticles. For a typical conjugation to a peptide, the peptide is dissolved in PBS (pH 7.4). The PEG-COOH is activated separately as described above, then added to the peptide solution. After incubation, purify the PEGylated peptide by HPLC or size exclusion. The PEGylated product can then be tested in cell-based assays for activity (e.g., receptor binding or signaling). However, the PEG linker itself is inert. For cell viability assays, the unreacted PEG (up to 10 mg/mL) shows no cytotoxicity in most cell lines. For research use, follow standard conjugation protocols.
Animal Protocol
Not applicable. The compound is not administered in vivo as a standalone agent. For a PEGylated drug candidate, the conjugate can be dosed in animals. For example, a PEG10k-anti-cancer peptide conjugate may be injected intravenously into tumor-bearing mice at 10-50 mg/kg. The PEG10k linker helps to extend the half-life of the peptide. In such studies, vehicle control groups might receive PBS. However, the unconjugated PEG is not administered. There is no standard in vivo protocol for HO-PEG-CH2COOH alone. For safety studies, PEG 10 kDa administered intravenously in rats at 1 g/kg causes transient renal vacuolation but is not lethal. For research, it is a conjugation reagent.
ADME/Pharmacokinetics
For PEG with MW 10,000 Da, the pharmacokinetics in rodents: after intravenous injection, the plasma half-life is 2-6 hours, which is shorter than that of 35 kDa PEG (days) because 10 kDa is closer to the renal filtration cutoff (≈30-40 kDa). In mice, the t1/2 of 10 kDa PEG is approximately 4-8 hours. The volume of distribution is low (≈50-100 mL/kg). It is not metabolized; it is excreted primarily in urine. The compound does not cross the blood-brain barrier. When conjugated to a drug, the PK of the conjugate is dominated by the PEG moiety. For PK analysis, quantify PEGylated drug by ELISA or LC-MS. The product is a reagent, not a drug; no internal PK data are required for research use.
Toxicity/Toxicokinetics
PEG 10,000 Da is generally recognized as safe (GRAS) for use in pharmaceutical formulations at low concentrations (<1% w/v). In preclinical toxicology, high doses (≥500 mg/kg i.v.) may cause mild renal tubular vacuolation in rats, which is reversible. No genotoxicity or carcinogenicity is associated with PEG. Acute toxicity is very low (LD50 >10 g/kg in rodents). The compound is not intended for human use as a drug; it is a research chemical. Standard safety precautions (gloves, lab coat) should be taken. Avoid ingestion and inhalation. This product is for research use only.
References

[1]. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.

Additional Infomation
HO-PEG-CH2COOH (MW 10000) is a heterobifunctional PEG linker widely used in bioconjugation and drug delivery. It allows for the attachment of drugs, peptides, and proteins via the carboxylic acid end (activated as NHS ester) while the hydroxyl end remains inert or can be further modified. Compared to the 35 kDa version, the 10 kDa PEG provides a shorter chain, which may be advantageous for certain applications (e.g., lower viscosity, easier characterization). The product is supplied as a white powder and should be stored dry at -20degC or 4degC. It is for research use only and is not an FDA-approved drug. It is a standard laboratory reagent.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Weight
10000.00
Appearance
Solid powder
HS Tariff Code
2934.99.9001
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.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO :~100 mg/mL (~10.00 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (0.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (0.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (0.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.1000 mL 0.5000 mL 1.0000 mL
5 mM 0.0200 mL 0.1000 mL 0.2000 mL
10 mM 0.0100 mL 0.0500 mL 0.1000 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.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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