化学性质：                                                                                                             

产品描述：                                                                                                            

BMS 195614 is a selective RARα antagonist [1]. It can bind to the RARα subunit [5].

BMS195614,4[[[[5,6-Dihydro-5,5-dimethyl-8-(3-quinolinyl)]-2-naphthalenyl] carbonyl]amino]benzoic acid [2], was considered to be retinoid antagonists as it inhibited all-transretinoic acid-induced (ATRA-induced) retinoic acid response elements-chloramphenicol acetyltransferase (RARE-CAT) reporter expression via concomitantly transfected retinoic acid receptors (RARs) [3][4].

Retinoic acids (RAs) are the most notably biologically active derivatives (collectively referred to as retinoids) of vitamin A (retinol). Retinoic acids exert a wide variety of profound effects on cellular differentiation, vertebrate development and homeostasis [6].

BMS 195614 reversed the induction effect of selective RARα agonists, AM580, AM80 and BMS 194753 on differentiation of the acute promyelocytic leukemia cell lines, NB4 and HL60 [1]. Treatment with retinoic acid (RA) (10-6 M) for 72 hrs significantly reduced T47D breast cancer cells migration. But RA in combination with BMS 195614 did not affect the cell movement [7]. In cells of a bovine stromal-vascular fraction from intramuscular fat, BMS 195614 significantly diminished the anti-adipogenic effect of ATRA [8].

BMS 195614 displayed poor in vivo activity in mice when administered orally. Treatment with BMS 195614 at oral doses for 1 month showed no inhibition to spermatogenesis [3]. Oral administration of BMS 195614 did not suppress spermatogenesis in mice [9].

特别提醒：