Table 1.
Ligand | Displays TRβ binding affinity (with respect to T3) | Reduces Plasma LDL cholesterol | Acts LDL receptor- dependent | Prevents hepatic steatosis | Causes insulin resistance | Increases heart weight/rate |
---|---|---|---|---|---|---|
THYROMIMETIC | ||||||
L-94901 | Weak | Yes | No | |||
CGS-23425 | Weak | Yes | No | |||
TRβ AGONIST | ||||||
GC-1 | Equal | Yes | No | Yes | Yes | No |
GC-24 | 2-fold lower | Yes | Yes | Yes | No | |
KB-141 | 6-fold lower | Yes | Yes | No | ||
T-0681 | Yes | Yes | No | |||
DITPA | Yes | Yes | No | |||
LIVER-TARGETED | ||||||
CGH-509A | Yes | No | ||||
MB-07811 | Yes | Yes | No | |||
MB-07344 | 2-fold lower | Yes | Yes | No | ||
KB-2115 | Yes | No | Yes | No | ||
TH METABOLITE | ||||||
TRIAC | 3-fold higher however no (or weak) TRβ specificity | No | ||||
T1AM | None | No | No | Yes | No | |
T2 | 60-fold lower (human TRβ) with no TRβ specificity | Yes | No | Yes | No (rats) | No/No (rats) |
ND (mice) | Yes/ND (mice)* |
Abbreviations: ND, not determined;
dose of T2 used in mice is 10-fold higher.