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AGN 193109 促销  ≥98%

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包装规格：5mg 10mg in glass bottle
溶解性：溶于DMSO（2 mg/mL 加热）
产品描述：基本信息 产品编号： A11325 产品名称： AGN 193109 CAS: 171746-21-7   储存条件 粉末 -20℃ 四年     分子式： C28H24O2 溶于液体 -80℃ 六个月 分子量 392.49 -20℃ 一个月 化学名：  4-{[5,5-diMethyl-8-(4-Methylphenyl)-5,6-dihydronaphthalen-2-yl]ethynyl}benzoic acid Solubility (25°C)：   体外:   DMSO 2mg/mL(5.10mM;Need warming) Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.5478mL 12.7392mL 25.4784mL 5mM 0.5096mL 2.5478mL 5.0957mL   生物活性 产品描述 一种视黄酸类似物，是有效的，特异性的视黄酸受体(RARs)拮抗剂，可抑制RARα，RARβ和RARγ的活性，Kd值分别为2nM，2nM和3nM。 靶点 Kd:2nM(RARα),2nM(RARβ),3nM(RARγ) 体外研究 AGN 193109 is a highly effective antagonist of retinoic acid receptors, with Kds of 2nM, 2nM, and 3nM for RARα, RARβ, and RARγ, respectively. AGN 193109 is completely RAR specific, because it does not bind to or transactivate through any of the RXRs. AGN 193109 (100nM) inhibits the TTNPB (a retinoic acid receptor agonist)-dependent morphological change in ECE16-1 cells. AGN193109 half-reverses retinoid-dependent growth suppression at 10nM, and completely shows this effect at 100nM in ECE16-1 cells. AGN193109 (100nM) also eliminates TTNPB-induced decrease in levels of K5, K6, K14, K16, and K17 and increase in levels of K7, K8, and K19 体内研究 AGN 193109 (1.15μmol/kg) does not causes overt toxicity and has no effect on spleen weight on the mice, but it suppresses TTNPB-induced increase in spleen weight of the mice. AGN 193109 also significantly reduces the cutaneous toxicity induced by ATRA. AGN 193109 (0.30 or 1.20μmol/kg) by topical treatment significantly reduces both weight loss and cutaneous toxicity caused by oral TTNPB cotreatment   推荐实验方法(仅供参考) Cell Assay Cells (10,000/cm2 ) are seeded in complete medium and allowed to attach overnight. The cells are then shifted to defined medium (DM), allowed to equilibrate for 24 h, and treatment is initiated by addition of fresh DM or DM containing epidermal growth factor (EGF) or retinoid. After 3 days of daily treatment with retinoid, the cells are harvested with 0.025% trypsin, 1mM EDTA, fixed in isotonic buffer containing 4% formaldehyde, and counted using a counter Animal Administration Mice (n=6) are treated topically on the dorsal skin with vehicle (92.5% acetone/7.5% DMSO), 0.072μmol/kg of TTNPB, 1.15μ mol/kg of AGN 193109, or 0.072μmol/kg of TTNPB plus 0.072, 0.288, or 1.15μmol/kg of AGN 193109 for 5 days. Mice are euthanized on Day 8
保存条件：-20℃

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