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Bi-steric inhibitor 16 undergoes ring opening of the rapamycin macrocycle in vivo to form ring-opened 32. (A) Mouse PK: male Balb/c mice (n = 3), IP = 3 mg/kg. (B) Rat PK: male Sprague–Dawley rats (n = 3), IV bolus = 1 mg/kg; vehicle = transcutol/solutol HS15/H2O 5%/5%/90% (v,w,v).
