Compounds and methods for determination of FKBP-binding immunosuppressant drugs

摘要

Compositions are disclosed for releasing an FKBP-binding immunosuppressant drug from endogenous binding substances in a sample suspected of containing the FKBP-binding immunosuppressant drug. The compositions include sirolimus derivatives that are modified with a bulky organic radical in the triene portion of the sirolimus molecule. The compositions may be employed in conjunction with assays for an FKBP-binding immunosuppressant drug in a sample suspected of containing the drug.

主权项

1. A composition for releasing an FKBP-binding immunosuppressant drug from endogenous binding substances in a sample suspected of containing the FKBP-binding immunosuppressant drug, the composition comprising:
(a) a compound of the formula: wherein: R1, R2 and R3 are each independently H or lower alkyl; R4 and R5 are each independently H, lower hydrocarbyl or lower hydrocarbyloxy or taken together to form a double bond to O, CH2, N-alkyl, or N—O-alkyl; R6 and R7 are each independently H, lower hydrocarbyl or lower hydrocarbyloxy or taken together to form a double bond to O, CH2, or N-alkyl, or N—O-alkyl; R8 and R9 are each independently H, non-bulky organic radical or a bulky organic radical, or are taken together to form a double bond to O or CH2; R10 and R11 are each independently H, non-bulky organic radical or a bulky organic radical, or are taken together to form a double bond to O or CH2; R12 is H, non-bulky hydrocarbyl or a bulky organic radical; wherein at least one of R8, R9, R10, R11 or R12 is a bulky organic radical; a is 0 or 1; and D is N, O, or CH, with the proviso that a is 0 when D is O; and
(b) a buffered medium.