Lipids

DSPE-PEG-TCO, MW 2,000 is a large PEG-lipid with a DSPE group and a trans-cyclooctyne moiety. DSPE is a phospholipid known for spontaneously forming micelles in aqueous media. DSPE-PEG conjugates are commonly used in the development of lipid nanoparticles in drug delivery. TCO is a click chemistry handle that is used with tetrazine-containing compounds for highly efficient labeling.

PEG3-bis(Amino-Tri-(Propargyl-PEG8-ethoxymethyl)-methane) is large molecule with two sets of three terminal alkynes joined together by a short PEG linker. The alkynes are most frequently used in copper click chemistry with azides to form stable triazoles with the target compound. The PEG linkers as well as numerous amide bonds provide high aqueous solubility to this compound, which may alter DMPK of this compound.

mPEG-DMG, MW 2,000 is a large PEG lipid containing a DMG group and a methoxy cap. The methoxy cap is inert while the DMG group is a popular component for developing lipid nanoparticles. Varying the size of a PEG linker greatly impacts its molecular dynamics, thereby affecting DMPK and ADME properties of a given API.

3-Amino-2-sulfopropanoic acid is a short molecule featuring a carboxylic acid, a sulfonate group, and a primary amine. The carboxylic acid and the primary amine are free to link this molecule to larger structures while the sulfonate group provides high water solubility to this aliphatic compound.

14-(Bromoacetamido-PEG6-ethylcarbamoyl)tridecanoic t-butyl ester is a bifunctional PEG linker containing a bromoacetamide, a PEG6 spacer, and a tridecanoic t-butyl ester. Bromoacetamide is a thiol-specific covalent ligand while the t-butyl ester can be hydrolyzed to allow for reactions with amines or alcohols to form amides or esters respectively.

Lipid 2 is an ionizable aminolipid featuring a dimethylamine headgroup, a thiocarbamate linking to a central amine with two ester branches, one unsaturated C9 and a saturated C17. This compound may be employed in the development of lipid nanoparticles for drug delivery.

t-Boc-N-amido-PEG-Succinimidyl Carbonate, MW 5,000 is a PEG reagent containing a Boc-protected amine and a succinimidyl carbonate. The carbonate is a strong leaving group, being easily substituted by nucleophiles such as amines and alcohols to form new carbamates or carbonates respectively. The Boc group can be deprotected by acidic conditions, which frees the amine to react with functional groups such as carboxylic acids, aldehydes and ketones.

PEG3-bis(Amino-Tri-(Acid-ethoxymethyl)-methane) is a PEG linker containing two sets of three carboxylic acids joined together by a short PEG spacer. The carboxylic acids are open for reactions with nucleophiles such as amines to form amides with a target compound. The PEG linker provides aqueous solubility.

PEG13-bis(Amino-Tri-(Acid-ethoxymethyl)-methane) is a hexafunctional PEG linker containing a pair of three carboxylic acids joined together by a PEG spacer. The carboxylic acids are free for coupling reactions with amines and alcohols. The long PEG spacer provides high aqueous solubility and alters DMPK.