m-dPEG®x-NHS ester

Amount: 100mg

Item Name: m-dPEG®8-NHS ester

Item #: 10260

Mol. Wt.: 509.54;

single compound dPEG® Spacer is 26 atoms and 29.8 A

Product Features and Benefits: Makes discrete MW pegylation modification possible with our unique range of m-dPEG® pegylation NHS esters m-dPEG® pegylation produces compounds with increased water solubility and reduced aggregation, also reduces immunogenicity and potentially even toxicity Can be used in conjunction with amino protected amino dPEG® acids for the pegylation of surfaces for produce hydrophilic and reactive surfaces with no non-specific binding issues Allows for low MW discrete pegylation of small molecule drugs and other related compounds for increased water solubility and reduced aggregation, or of surfaces to reduce non-specific binding; may even be useful for “dusting” enzymes and other proteins to increase chemical stability Amine reactive Produces stable amide bond General Protocol for modification: The amount of the m-dPEGx® NHS ester used in the modification reaction is potentially going to depend on several variables, including, a) the modification application, e.g., solution or surface, organic or aqueous, large biological or small organic, b) the concentration of the specific reactive amines available for reaction, as well as c) the desired effect from the m-dPEG® which is incorporated. In this latter case, choosing the proper value of x will be important, and this may involve experimenting with a range of values, currently from x = 2 to 24, as well as a tribranched compound with a discrete MW over 2200 D. Therefore, one needs to take at least these variables into consideration before a basic optimization experiment is designed and run. m-dPEG®x NHS Pegylation modification reaction

Protocol: a) For aqueous based modifications the reaction can be run in an amine-free buffer at pH 7-8. The m-dPEG® NHS ester can be added as a stock solution in a dry organic solvent such as DMAC (recommended), DMSO or DMF. This stock solution can be stored for several months frozen at –20°C, if care is taken to exclude moisture in the preparation and handling of the NHS ester. The calculated amount of the stock is added to the aqueous reactant solution and the reaction will be complete in about 30 minutes to about 2 hours, depending on the specific stoichiometry of the reaction and the desired extent of reaction. The half-life of the NHS ester at pH 8 and 4°C is about 60 minutes. Use your established methods to monitor the reaction. b) For organic based modifications one uses standard organic procedures, generally adding a solution of the m-dPEG® NHS ester to a solution of the reactant containing a tertiary amine, e.g., Hünig’s base, triethylamine. Homogeneous reactions are typically monitored by TLC or HPLC. Where possible we recommend using methylene chloride as the reaction solvent, which also greatly facilitates the work-up, however, if the solubility of the compound to be modified will not allow this, use other appropriate solvents like DMF or DMAC. Optionally, the reaction can be run as a slurry and the reaction will “pull” the reactants into solution, as the incorporated dPEG™ will greatly increase the solubility in many organic solvents, but especially methylene chloride.

Amount: 100mg

Item Name: m-dPEG®24-NHS ester

Item #: 10304

Mol. Wt.: 1214.39;

single compound dPEG® Spacer is 74 atoms and 86.2 A

Product Features and Benefits: Makes discrete MW pegylation modification possible with our unique range of m-dPEG® pegylation NHS esters m-dPEG® pegylation produces compounds with increased water solubility and reduced aggregation, also reduces immunogenicity and potentially even toxicity Can be used in conjunction with amino protected amino dPEG® acids for the pegylation of surfaces for produce hydrophilic and reactive surfaces with no non-specific binding issues Allows for low MW discrete pegylation of small molecule drugs and other related compounds for increased water solubility and reduced aggregation, or of surfaces to reduce non-specific binding; may even be useful for “dusting” enzymes and other proteins to increase chemical stability Amine reactive Produces stable amide bond General Protocol for modification: The amount of the m-dPEG®x NHS ester used in the modification reaction is potentially going to depend on several variables, including, a) the modification application, e.g., solution or surface, organic or aqueous, large biological or small organic, b) the concentration of the specific reactive amines available for reaction, as well as c) the desired effect from the m-dPEG® which is incorporated. In this latter case, choosing the proper value of x will be important, and this may involve experimenting with a range of values, currently from x = 2 to 24, as well as a tribranched compound with a discrete MW over 2200 D. Therefore, one needs to take at least these variables into consideration before a basic optimization experiment is designed and run. m-dPEG®x NHS Pegylation modification reaction

Protocol: a) For aqueous based modifications the reaction can be run in an amine-free buffer at pH 7-8. The m-dPEG® NHS ester can be added as a stock solution in a dry organic solvent such as DMAC (recommended), DMSO or DMF. This stock solution can be stored for several months frozen at –20°C, if care is taken to exclude moisture in the preparation and handling of the NHS ester. The calculated amount of the stock is added to the aqueous reactant solution and the reaction will be complete in about 30 minutes to about 2 hours, depending on the specific stoichiometry of the reaction and the desired extent of reaction. The half-life of the NHS ester at pH 8 and 4°C is about 60 minutes. Use your established methods to monitor the reaction. b) For organic based modifications one uses standard organic procedures, generally adding a solution of the m-dPEG® NHS ester to a solution of the reactant containing a tertiary amine, e.g., Hünig’s base, triethylamine. Homogeneous reactions are typically monitored by TLC or HPLC. Where possible we recommend using methylene chloride as the reaction solvent, which also greatly facilitates the work-up, however, if the solubility of the compound to be modified will not allow this, use other appropriate solvents like DMF or DMAC. Optionally, the reaction can be run as a slurry and the reaction will “pull” the reactants into solution, as the incorporated dPEG® will greatly increase the solubility in many organic solvents, but especially methylene chloride.

Amount: 100mg

Item Name: m-dPEG®2-NHS ester

Item #: 10327

Mol. Wt.: 245.23;

single compound dPEG® Spacer is 8 atoms and 8.5 A

Product Features and Benefits: Makes discrete MW pegylation modification possible with our unique range of m-dPEG® pegylation NHS esters m-dPEG® pegylation produces compounds with increased water solubility and reduced aggregation, also reduces immunogenicity and potentially even toxicity Can be used in conjunction with amino protected amino dPEG® acids for the pegylation of surfaces for produce hydrophilic and reactive surfaces with no non-specific binding issues Allows for low MW discrete pegylation of small molecule drugs and other related compounds for increased water solubility and reduced aggregation, or of surfaces to reduce non-specific binding; may even be useful for “dusting” enzymes and other proteins to increase chemical stability Amine reactive Produces stable amide bond General Protocol for modification: The amount of the m-dPEG®x NHS ester used in the modification reaction is potentially going to depend on several variables, including, a) the modification application, e.g., solution or surface, organic or aqueous, large biological or small organic, b) the concentration of the specific reactive amines available for reaction, as well as c) the desired effect from the m-dPEG® which is incorporated. In this latter case, choosing the proper value of x will be important, and this may involve experimenting with a range of values, currently from x = 2 to 24, as well as a tribranched compound with a discrete MW over 2200 D. Therefore, one needs to take at least these variables into consideration before a basic optimization experiment is designed and run. m-dPEG®x NHS Pegylation modification reaction

Protocol: a) For aqueous based modifications the reaction can be run in an amine-free buffer at pH 7-8. The m-dPEG® NHS ester can be added as a stock solution in a dry organic solvent such as DMAC (recommended), DMSO or DMF. This stock solution can be stored for several months frozen at –20°C, if care is taken to exclude moisture in the preparation and handling of the NHS ester. The calculated amount of the stock is added to the aqueous reactant solution and the reaction will be complete in about 30 minutes to about 2 hours, depending on the specific stoichiometry of the reaction and the desired extent of reaction. The half-life of the NHS ester at pH 8 and 4°C is about 60 minutes. Use your established methods to monitor the reaction. b) For organic based modifications one uses standard organic procedures, generally adding a solution of the m-dPEG® NHS ester to a solution of the reactant containing a tertiary amine, e.g., Hünig’s base, triethylamine. Homogeneous reactions are typically monitored by TLC or HPLC. Where possible we recommend using methylene chloride as the reaction solvent, which also greatly facilitates the work-up, however, if the solubility of the compound to be modified will not allow this, use other appropriate solvents like DMF or DMAC. Optionally, the reaction can be run as a slurry and the reaction will “pull” the reactants into solution, as the incorporated dPEG® will greatly increase the solubility in many organic solvents, but especially methylene chloride.

Amount: 100mg

Item Name: m-dPEG®49-NHS ester

Item #: 10920

Mol. Wt.: 2232.65;

single compound dPEG® Spacer is 177.7 atoms and 150 A

Product Features and Benefits: Makes discrete MW pegylation modification possible with our unique range of m-dPEG® pegylation NHS esters m-dPEG® pegylation produces compounds with increased water solubility and reduced aggregation, also reduces immunogenicity and potentially even toxicity Can be used in conjunction with amino protected amino dPEG® acids for the pegylation of surfaces for produce hydrophilic and reactive surfaces with no non-specific binding issues Allows for low MW discrete pegylation of small molecule drugs and other related compounds for increased water solubility and reduced aggregation, or of surfaces to reduce non-specific binding; may even be useful for “dusting” enzymes and other proteins to increase chemical stability Amine reactive Produces stable amide bond General Protocol for modification: The amount of the m-dPEG®x NHS ester used in the modification reaction is potentially going to depend on several variables, including, a) the modification application, e.g., solution or surface, organic or aqueous, large biological or small organic, b) the concentration of the specific reactive amines available for reaction, as well as c) the desired effect from the m-dPEG® which is incorporated. In this latter case, choosing the proper value of x will be important, and this may involve experimenting with a range of values, currently from x = 2 to 24, as well as a tribranched compound with a discrete MW over 2200 D. Therefore, one needs to take at least these variables into consideration before a basic optimization experiment is designed and run. m-dPEG®x NHS Pegylation modification reaction

Protocol: a) For aqueous based modifications the reaction can be run in an amine-free buffer at pH 7-8. The m-dPEG® NHS ester can be added as a stock solution in a dry organic solvent such as DMAC (recommended), DMSO or DMF. This stock solution can be stored for several months frozen at –20°C, if care is taken to exclude moisture in the preparation and handling of the NHS ester. The calculated amount of the stock is added to the aqueous reactant solution and the reaction will be complete in about 30 minutes to about 2 hours, depending on the specific stoichiometry of the reaction and the desired extent of reaction. The half-life of the NHS ester at pH 8 and 4°C is about 60 minutes. Use your established methods to monitor the reaction. b) For organic based modifications one uses standard organic procedures, generally adding a solution of the m-dPEG® NHS ester to a solution of the reactant containing a tertiary amine, e.g., Hünig’s base, triethylamine. Homogeneous reactions are typically monitored by TLC or HPLC. Where possible we recommend using methylene chloride as the reaction solvent, which also greatly facilitates the work-up, however, if the solubility of the compound to be modified will not allow this, use other appropriate solvents like DMF or DMAC. Optionally, the reaction can be run as a slurry and the reaction will “pull” the reactants into solution, as the incorporated dPEG® will greatly increase the solubility in many organic solvents, but especially methylene chloride.