The present invention provides a long chain fatty acid (LCFA)-like albumin-binding probe/ligand containing no hydrolysable bond and having an enhanced associating affinity with human serum albumin, which upon conjugation with an amino- or mercapto-containing short-lived drug and administration of the conjugate, significantly prolongs the life time of said drug without substantially interfering with its pharmacological activity. The invention further provides conjugates of said probe with amino- or mercapto-containing drugs, as well as pharmaceutical compositions and uses thereof.