Table 1.

From thyromimetics to TRβ ligands and TH metabolites: reported TRβ affinities and metabolic effects.

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.