PEGylation and Activated PEGs
Activated PEGs
Linear Activated PEGs
With our sophisticated experience of synthesis and our purification technology, NOF provides high-quality activated PEGs based on high-quality mPEG. NOF’s activated PEGs contain low levels of impurities such as bifunctional PEGs derived from diols in the mPEG. The freedom from diol impurities means that undesirable crosslinking of drugs during PEG modification can be completely suppressed.
CH3O(CH2CH2O)nX (X = reactive group) |
|
| Product | Reactive Group | Target Group |
| CS series |
-CO-CH2CH2-COO-NHS* | -NH2,-OH,-SH |
| GS series |
-CO-CH2CH2CH2-COO-NHS* | -NH2,-OH,-SH |
| AS series |
-CH2-COO-NHS* | -NH2,-OH,-SH |
| HS series |
-CH2CH2CH2CH2CH2-COO-NHS* | -NH2,-OH,-SH |
| NP series |
-CO2-p-C6H4-NO2 | -NH2 |
| AL series |
-CH2CH2-CHO | -NH2 |
| PA series |
-CH2CH2CH2NH2 | -COOH |
| DE series |
-CH2CH2CH(OC2H5)2 | -NH2 |
| SH series |
-CH2CH2SH- | SH,-N-Maleimidyl,-COOH |
| MA series |
-CH2CH2CH2NHCOCH2CH2-N-Maleimidyl | -SH |
SUNBRIGHT® CS, GS, AS, and HS Series (Carboxylated-mPEGs; NHS active esters)
NOF provides four types of linkage between the PEG chain and the N-succinimidyl (NHS) group. Customers can therefore choose appropriate products according to their needs and the desired stability of the PEGylated drug.
Succinate X = -COCH2CH2COO-
| Product Name | Description |
| SUNBRIGHT® ME-020CS |
mPEG-succinyl-NHS, MW 2000 |
| SUNBRIGHT® ME-050CS |
mPEG-succinyl-NHS, MW 5000 |
Glutarate X =-COCH2CH2 CH2COO-
| Product Name | Description |
| SUNBRIGHT® MEGC-050HS |
mPEG-glutaryl-NHS, MW 5000 |
| SUNBRIGHT® MEGC-20TS |
mPEG-glutaryl-NHS, MW 20,000 |
| SUNBRIGHT® MEGC-30TS |
mPEG-glutaryl-NHS, MW 30,000 |
Carboxymethyl X =-CH2COO-
| Product Name | Description |
| SUNBRIGHT® ME-020AS |
mPEG-carboxymethyl-NHS, MW 2000 |
| SUNBRIGHT® ME-050AS |
mPEG-carboxymethyl-NHS, MW 5000 |
Carboxypentyl X =-(CH2)5COO-
| Product Name | Description |
| SUNBRIGHT® ME-050HS |
mPEG-carboxyheptyl-NHS, MW 5000 |
| SUNBRIGHT® ME-200HS |
mPEG-carboxyheptyl-NHS, MW 20,000 |
SUNBRIGHT® NP Series (p-Nitrophenyl-PEGs)
| Product Name | Description |
| SUNBRIGHT® MENP-20H |
mPEG-nitrophenylcarbonate, MW 2000 |
| SUNBRIGHT® MENP-50H |
mPEG-nitrophenylcarbonate, MW 5000 |
| SUNBRIGHT® MENP-10T |
mPEG-nitrophenylcarbonate, MW 10,000 |
| SUNBRIGHT® MENP-20T |
mPEG-nitrophenylcarbonate, MW 20,000 |
| SUNBRIGHT® MENP-30T |
mPEG-nitrophenylcarbonate, MW 30,000 |
SUNBRIGHT® AL Series
NOF owns rights to state-of-the-art synthetic methods for making amine-reactive mPEG-aldehydes that avoid the formation of common bifunctional impurities.
| Product Name | Description |
| SUNBRIGHT® ME-050AL |
mPEG-propylaldehyde, MW 5000 |
| SUNBRIGHT® ME-100AL |
mPEG-propylaldehyde, MW 10,000 |
| SUNBRIGHT® ME-200AL |
mPEG-propylaldehyde, MW 20,000 |
| SUNBRIGHT® ME-300AL |
mPEG-propylaldehyde, MW 30,000 |
SUNBRIGHT® PA Series (Amino-PEGs)
NOF offers propylamine-functionalized amino-terminal PEGs.
| Product Name | Description |
| SUNBRIGHT® MEPA-020H |
mPEG-propylamine, MW 2000 |
| SUNBRIGHT® MEPA-050H |
mPEG-propylamine, MW 5000 |
| SUNBRIGHT® MEPA-12T |
mPEG-propylamine, MW 12,000 |
| SUNBRIGHT® MEPA-20T |
mPEG-propylamine, MW 20,000 |
| SUNBRIGHT® MEPA-30T |
mPEG-propylamine, MW 30,000 |
SUNBRIGHT® SH Series (Thiol-PEGs)
| Product Name | Description |
| SUNBRIGHT® ME-020SH |
mPEG-thiol, MW 2000 |
| SUNBRIGHT® ME-050SH |
mPEG-thiol, MW 5000 |
| SUNBRIGHT® ME-100SH |
mPEG-thiol, MW 10,000 |
| SUNBRIGHT® ME-200SH |
mPEG-thiol, MW 20,000 |
| SUNBRIGHT® ME-300SH |
mPEG-thiol, MW 30,000 |
SUNBRIGHT® MA Series (Maleimidyl-PEGs))
NOF offers high-quality maleimide-functionalized PEGs.
| Product Name | Description |
| SUNBRIGHT® ME-020MA |
mPEG-maleimide, MW 2000 |
| SUNBRIGHT® ME-050MA |
mPEG-maleimide, MW 5000 |
| SUNBRIGHT® ME-120MA |
mPEG-maleimide, MW 12,000 |
| SUNBRIGHT® ME-200MA |
mPEG-maleimide, MW 20,000 |
| SUNBRIGHT® ME-300MA |
mPEG-maleimide, MW 30,000 |
Bifunctional PEG Series
NOF produces multi-arm activated PEGs and multi-functional PEG derivatives (bifunctional, trifunctional, quadrifunctional, octafunctional, and heterofunctional) in a wide variety of molecular weights, according to customers' needs.
X = (N-Succinimidyloxycarbonyl)methyl, ( —CH2COO-NHS)
| Product Name | Description |
| SUNBRIGHT® DE-034AS* |
PEG-dicarboxymethyl NHS, MW 3400 |
X = (N-Succinimidyloxycarbonyl)propyl, ( —CH2CH2CH2COO-NHS)
| Product Name | Description |
| SUNBRIGHT® DE-034GS |
PEG-diglutarateNHS, MW 3400 |
| SUNBRIGHT® DE-100GS |
PEG-diglutarateNHS, MW 10,000 |
| SUNBRIGHT® DE-200GS |
PEG-diglutarateNHS, MW 20,000 |
X = (N-Succinimidyloxycarbonyl)pentyl, ( —(CH2)5COO-NHS)
| Product Name | Description |
| SUNBRIGHT® DE-034HS |
PEG-dicarboxyheptylNHS, MW 3400 |
| SUNBRIGHT® DE-100HS |
PEG-dicarboxyheptylNHS, MW 10,000 |
| SUNBRIGHT® DE-200HS |
PEG-dicarboxyheptylNHS, MW 20,000 |
X = 3-(N-Maleimidyl)propanamido, ( —(NHCOCH2CH2-MAL)
| Product Name | Description |
| SUNBRIGHT® DE-100MA |
PEG-dimaleimide, MW 10,000 |
| SUNBRIGHT® DE-200MA |
PEG-dimaleimide, MW 20,000 |
X = Aminopropyl,( —CH2CH2CH2NH2)
| Product Name | Description |
| SUNBRIGHT® DE-034PA |
PEG-dipropylamine, MW 3400 |
| SUNBRIGHT® DE-100PA |
PEG-dipropylamine, MW 10,000 |
| SUNBRIGHT® DE-200PA |
PEG-dipropylamine, MW 20,000 |
| SUNBRIGHT® DE-300PA |
PEG-dipropylamine, MW 30,000 |
X = 2-Sulfanylethyl, ( —CH2CH2SH)
| Product Name | Description |
| SUNBRIGHT® DE-050SH |
PEG-dithiol, MW 5000 |
| SUNBRIGHT® DE-100SH |
PEG-dithiol, MW 10,000 |
| SUNBRIGHT® DE-200SH |
PEG-dithiol, MW 20,000 |
Four-Armed Functional PEG Series
X = 3-(N-Succinimidyloxycarbonyl)propyl, ( —CH2CH2CH2COO-NHS)
| Product Name | Description |
| SUNBRIGHT® PTE-100GS |
PEG-tetraglutaryl NHS, MW 10,000 |
| SUNBRIGHT® PTE-200GS |
PEG-tetraglutaryl NHS, MW 20,000 |
X = 5-(N-Succinimidyloxycarbonyl)pentyl, [ —(CH2)5COO-NHS]
| Product Name | Description |
| SUNBRIGHT® PTE-200HS |
PEG-dicarboxyheptyl NHS, MW 20,000 |
X = p-Nitrophenyloxycarbonyl, ( —CO2-p-C6H4NO2)
| Product Name | Description |
| SUNBRIGHT® PTE-100NP |
PEG-tetranitrophenylcarbonate, MW 10,000 |
| SUNBRIGHT® PTE-200NP |
PEG-tetranitrophenylcarbonate, MW 20,000 |
X = 3-(N-Maleimido)propanamido ( —NHCOCH2CH2-MAL)
| Product Name | Description |
| SUNBRIGHT® PTE-200MA* |
PEG-tetramaleimide, MW 20,000 |
X = 3-Aminopropyl ( —CH2CH2CH2NH2)
| Product Name | Description |
| SUNBRIGHT® PTE-100PA |
PEG-tetrapropylamine, MW 10,000 |
| SUNBRIGHT® PTE-200PA |
PEG-tetrapropylamine, MW 20,000 |
X = 2-Sulfanylethyl, ( —CH2CH2SH)
| Product Name | Description |
| SUNBRIGHT® PTE-100SH |
PEG-tetrathiol. MW 10,000 |
| SUNBRIGHT® PTE-200SH |
PEG-tetrathiol. MW 20,000 |
Eight-Arm Functional PEG Series
X = 3-(N-Succinimidyloxycarbonyl)propyl ( —CH2CH2CH2COO-NHS)
| Product Name | Description |
| SUNBRIGHT® HGEO-200GS |
PEG-octaglutaryl NHS, MW 20,000 |
X = (p-Nitrophenyl)oxycarbonyl ( —CO2C6H4NO2)
| Product Name | Description |
| SUNBRIGHT® HGEO-200NP |
PEG-octanitrophenylcarbonate, MW 20,000 |
Branched Activated PEGs
NOF has developed novel branched PEG products for sustained-release PEGylated drugs.
NOF offers various types of functional group, such as aldehyde, maleimide, carbonate, or carboxylate activated esters (Y), for activated branched PEGs. A range of spacers (X) for each functional group is also available. NOF's branched PEGs are our original and patented products. Please contact us for more detailed information about these branched PEGs.
| Product Name | Y: Functional Group | MW |
| SUNBRIGHT® GL2-400MA |
Maleimide | 40,000 |
| SUNBRIGHT® GL2-400PA |
Amine | 40,000 |
| SUNBRIGHT® GL2-400GS2 |
glutaryl-NHS | 40,000 |
| SUNBRIGHT® GL2-400TS |
Carbonate-NHS | 40,000 |
| SUNBRIGHT® GL2-400NP |
Carbonate-p-Nitrophenol | 40,000 |
Advantage of NOF's Branched PEGs
| Branched PEG modification offers the ability to customize bioactive agents and surfaces site-selectively with dual PEG chains for each site, as illustrated. The many choices of branched PEGs that are available will give you a greater chance of success in your drug-development efforts. |  |
Heterofunctional PEGs
NOF offers several high-purity heterofunctional PEGs.
Hydroxyl-PEG-Amine
| Product Name | Description |
| SUNBRIGHT® HO-020PA |
Hydroxyl-PEG-propylamine, MW 2000 |
| SUNBRIGHT® HO-034PA |
Hydroxyl-PEG-propylamine, MW 3400 |
| SUNBRIGHT® HO-050PA |
Hydroxyl-PEG-propylamine, MW 5000 |
Amino-PEG-Carboxylic acid
| Product Name | Description |
| SUNBRIGHT® PA-020HC |
Propylamine-PEG-carboxylic acid, MW 2000 |
| SUNBRIGHT® PA-034HC |
Propylamine-PEG-carboxylic acid, MW 3400 |
| SUNBRIGHT® PA-050HC |
Propylamine-PEG-carboxylic acid, MW 5000 |
Boc*-protected-Amino-PEG-Carboxyl-NHS
| Product Name | Description |
| SUNBRIGHT® BO-050TS |
Boc-PEG-carbonateNHS, MW 5000 |
Maleimide-PEG-Carboxyl-NHS
| Product Name | Description |
| SUNBRIGHT® MA-050TS* |
Maleimide-PEG-carbonate NHS, MW 5000 |
Hydroxy-PEG-Aldehyde
| Product Name | Description |
| SUNBRIGHT® HO-050AL |
Hydroxyl-PEG-propylaldehyde, MW 5000 |
| SUNBRIGHT® HO-100AL |
Hydroxyl-PEG-propylaldehyde, MW 10,000 |
| SUNBRIGHT® HO-200AL |
Hydroxyl-PEG-propylaldehyde, MW 20,000 |
| SUNBRIGHT® HO-300AL |
Hydroxyl-PEG-propylaldehyde, MW 30,000 |
Comb-Shaped Copolymers
These alternating copolymers have been developed to permit the introduction of a number of reactive anhydride groups and PEG chains into a single polymeric molecule (a comb-shaped polymer) as shown below.
When such polymers react with proteins or enzymes, a number of PEG chains can be introduced into the biomolecule or drug, as shown below. Moreover, the hydrophilic/lipophilic balance of the polymer can be controlled by changing the ratio of propylene oxide to ethylene oxide in the copolymer. By selecting appropriate polymers, custom-modified proteins, enzymes, or drugs can be produced that dissolve and are stabilized in organic solvents.
General Characteristics for PEG SUNBRIGHT® AM series
| Method of Test | AM-0530K | AM-1510K | AM-2090P |
| Mw of AO (PEG) |
about 500 | about 1,500 | about 2,000 |
| DP* |
about 30-40 | about 10-15 | about 10-20 |
| Total Mw |
about 15,000-20,000 | about 15,000-20,000 | about 20,000-40,000 |
   
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