Table 3: Selective PPAR γ modulators (SPPAR γMs).


name structure type

PAM-1616 [ 236 ] - partial agonist - fully dissociates co-repressors
KR62980 [ 237 ] - partial agonist
SPPARγM5 [ 238 ] - partial agonist
INT131 [ 239 , 240 ][ 244 ] - partial agonist - 40% transactivation compared to rosiglitazone
L312 [ 241 ] - partial agonist - blocks Cdk-5 mediated PPAR γ-phosphorylation
MK-0533 [ 242 ] - partial agonist
MBX-102 [ 243 ] - partial agonist - fully dissociates co-repressors - full efficacy in transrepression
S26948 [ 245 ] - only recruits GRIP1 in vitro - does not promote adipocyte differentiation and weight-gain
FK614 [ 246 , 247 ] - fully dissociates co-repressors - specific profile of co-activator recruitment - promotes adipogenesis
LG100641 [ 248 ] - antagonist - tissue/cell-type specific?
SR1664 [ 249 ] - non-agonist - blocks phosphorylation at Ser-273
GQ16 [ 252 ] - partial agonist - blocks phosphorylation at Ser-273