Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AGN 193109 是一种类视黄醇类似物,是一种有效的特异性 RAR 拮抗剂,可抑制 RARα、RARβ和 RARγ的活性,Kd 值分别为 2 nM、2 nM 和 3 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 663 | 现货 | ||
2 mg | ¥ 963 | 现货 | ||
5 mg | ¥ 1,580 | 现货 | ||
10 mg | ¥ 2,490 | 现货 | ||
25 mg | ¥ 4,260 | 现货 | ||
50 mg | ¥ 6,070 | 现货 | ||
100 mg | ¥ 8,370 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,770 | 现货 |
产品描述 | AGN 193109, a retinoid analog, is a potent and specific antagonist of RARs (Kds: 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ). |
靶点活性 | RARβ:2 nM (Kd), RARγ:3 nM (Kd), RARα:2 nM (Kd) |
体外活性 | AGN 193109 is completely RAR specific because it does not bind to or transactivate through any of the RXRs [1]. AGN 193109 (100 nM) inhibits the TTNPB (a retinoic acid receptor agonist)-dependent morphological change in ECE16-1 cells. AGN193109 half-reverses retinoid-dependent growth suppression at 10 nM, and completely shows this effect at 100 nM in ECE16-1 cells. AGN193109 (100 nM) also eliminates TTNPB-induced decrease in levels of K5, K6, K14, K16, and K17 and increases in levels of K7, K8, and K19 [2]. |
体内活性 | AGN 193109 (0.30 or 1.20 μmol/kg) by topical treatment significantly reduces both weight loss and cutaneous toxicity caused by oral TTNPB cotreatment. AGN 193109 (1.15 μmol/kg) does not cause 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 [3]. |
细胞实验 | 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 the 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, 1 mM EDTA, fixed in isotonic buffer containing 4% formaldehyde, and counted using a counter [2]. |
动物实验 | Mice (n=6) are treated topically on the dorsal skin with vehicle (92.5% acetone/7.5% DMSO), 0.072 μmol/kg of TTNPB, 1.15 μmol/kg of AGN 193109, or 0.072 μmol/kg of TTNPB plus 0.072, 0.288, or 1.15 μmol/kg of AGN 193109 for 5 days. Mice are euthanized on Day 8 [3]. |
分子量 | 392.49 |
分子式 | C28H24O2 |
CAS No. | 171746-21-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 3.92 mg/mL (10 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5478 mL | 12.7392 mL | 25.4784 mL | 63.6959 mL |
5 mM | 0.5096 mL | 2.5478 mL | 5.0957 mL | 12.7392 mL | |
10 mM | 0.2548 mL | 1.2739 mL | 2.5478 mL | 6.3696 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AGN 193109 171746-21-7 Autophagy Metabolism Retinoid Receptor Inhibitor Retinoic acid receptors Retinoid X receptors RAR/RXR AGN193109 inhibit AGN-193109 inhibitor