Synonyms: 4-[2-[4-(4-Ethylphenyl)-2,2-dimethyl-2H-1-benzothiopyran-6-yl]ethynyl]benzoic acid; 4-[[4-(4-Ethylphenyl)-2,2-dimethyl-2H-1-benzothiopyran-6-yl]ethynyl]benzoic acid; AGN 194310; AGN-194310; IRX4310; VTP 194310
Molecular Formula: C28H24O2S
Molecular Weight: 424.55
Linear Structural Formula: C28H24O2S
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: AGN194310 (IRX4310; VTP 194310) is a retinoic acid receptor (RAR) antagonist that targets all three RAR subtypes with higher affinity (RARalpha/beta/gamma Kd = 3/2/5 nM) than all-trans retinoic acid/ATRA (RARalpha/beta/gamma Kd = 15/13/18 nM) without affecting RXR subtypes. AGN194310 effectively blocks RAR agonist TTNPB-induced transcription activity (using RARalpha, RARbeta, or RARgamma transfected cells) and prevents TTNPB toxicity in guinea pigs in vivo (by 79/84/94% at AGN194310/TTNPB ratios of 0.5/2/8). AGN194310 potentiates differentiation in osteoblast cultures (1 muM) and daily oral administration (0.5 mg/kg/d for a10-d period) is reported to cause impaired radial bone growth among 8-wk-old mice.