CAS NO: | 182135-66-6 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
Cas No. | 182135-66-6 |
别名 | BMS 614 |
化学名 | 4-(5,5-dimethyl-8-(quinolin-3-yl)-5,6-dihydronaphthalene-2-carboxamido)benzoic acid |
Canonical SMILES | CC1(CC=C(C2=C1C=CC(C(NC3=CC=C(C(O)=O)C=C3)=O)=C2)C4=CC5=CC=CC=C5N=C4)C |
分子式 | C29H24N2O3 |
分子量 | 448.51 |
溶解度 | DMF: 30 mg/ml;DMSO: 30 mg/ml;DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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]. References: |