Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TTNPB (Ro 13-7410,AGN-191183) 是一种RAR 激动剂。在使用人RARs 进行竞争性结合实验中,作用于RARα,RARβ和RARγ,IC50分别为 5.1 nM,4.5 nM 和 9.3 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 219 | 现货 | ||
2 mg | ¥ 303 | 现货 | ||
5 mg | ¥ 663 | 现货 | ||
10 mg | ¥ 963 | 现货 | ||
25 mg | ¥ 1,770 | 现货 | ||
50 mg | ¥ 2,970 | 现货 | ||
100 mg | ¥ 4,380 | 现货 | ||
500 mg | ¥ 9,170 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 728 | 现货 |
产品描述 | TTNPB (Ro 13-7410,AGN-191183), a potent RAR agonist, inhibits binding of [3H]tRA of human RARα (IC50: 5.1 nM), β (IC50: 4.5 nM), and γ (IC50: 9.3 nM), respectively. |
靶点活性 | RARβ:4.5 nM, RARγ:9.3 nM, RARα:5.1 nM |
体外活性 | 通过诱导细胞凋亡,TTNPB(0.25 mg/kg)可抑制MXT-HI和MXT-HS模型的生长. |
体内活性 | 在条件培养基培养72 h,TTNPB可使JEG-3细胞中小鼠mRARα(EC50:2.0 nM)、β(EC50:1.1 nM)以及γ(EC50:0.8 nM)转录活性增加。TTNPB与核视黄酸受体的结合亲和力较高,从而抑制[3H]tRA与mRARα(IC50:3.8 nM)、 β(IC50:4.0 nM)以及γ(IC50:4.5 nM)的结合。通过诱导G1细胞周期阻滞,TTNPB对雌激素受体-阳性乳腺癌细胞和正常人体乳腺上皮细胞的生长具有抑制作用。TTNPB浓度依赖性地减少ES-D3细胞分化。 |
激酶实验 | Binding assays: Binding assays are performed as previously described (Allenby et al., 1993, 1994). Briefly, labeled and unlabeled retinoids are added to nucleosol or cytosolic fractions in ethanol so that the total amount of ethanol added is constant in all tubes and did not exceed 2% of the incubation volume. The receptor preparations are incubated with retinoids at 4°C for 4–6 hr. Sephadex PD-10 desalting columns are used to separate bound radioligand from free radioligand after equilib- rium is achieved. For competitive binding assays, varying concentrations of unlabeled competing ligand are incubated with the appropriate nucleosol or cytosol in the presence of a fixed concentration of [3H]tRA (sp. act. 49.3 Ci/mmol) or [3H]9-cis RA (sp. act. 24.0 Ci/mmol). Final concentrations of [3H] tRA and [3H]9-cis RA for nuclear receptor binding assays are 5 nM. Final concentrations of [3H] tRA for CRABP binding assays is 30 nM. The IC50s are calculated as described above (DeLean et al., 1978). For saturation kinetics, increasing concentrations of radiolabeled ligand ([3H]tRA sp. act. 49.3 Ci/mmol, [3H]TTNPB sp. act. 5.5 Ci/ mmol) are added to the nucleosol of the appropriate receptor subtype in the presence (nonspecific binding) or absence (total binding) of a 100-fold molar excess of the corresponding unlabeled retinoid. Specific binding is defined as the total binding minus nonspecific binding. Saturation kinetics are calculated as previously described (Scatchard, 1949; Grippo and Gudas, 1987; Levin et al., 1992). |
细胞实验 | Human mammary epithelial cells are maintained in Mammary Epithelial Basal Medium (MEBM) supplemented with the Mammary Epithelial Growth Media (MEGM) bullet kit. 184 and 184B5 cells are maintained in MEBM sodium-bicarbonate free (MEBM-SBF) supplemented with the MEGM bullet kit, isoproterenol (10 μM), and transferrin (5 μg/ml). MCF10A cell lines are maintained in DME/F12 containing 5% heat inactivated horse serum, penicillin/streptomycin (100 μg/ml and 100 μg/ml), hydrocortisone (1.4 μM), insulin (10 μg/ml), choleratoxin (100 ng/ml), and EGF (20 ng/ml). Breast cancer cell lines are maintained in Improved MEM Zinc Option containing 10% fetal bovine serum, 1% glutamine, and 1% penicillin/streptomycin. For growth assays, cells are treated with the different retinoids for the specified number of days with media and treatment changes every other day in T47D cells and every 2 days in 184 cells. Cell proliferation is measured according to the protocol for the CellTiter 96 Aqueous Non-Radioactive Cell Proliferation Assay. This colorimetric assay determines the number of viable cells in a sample. Each point represents samples done in quadruplicate.(Only for Reference) |
别名 | AGN191183, Arotinoid acid, Ro 13-7410,AGN-191183, Ro 13-7410 |
分子量 | 348.48 |
分子式 | C24H28O2 |
CAS No. | 71441-28-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 3.5 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 | 2.8696 mL | 14.348 mL | 28.6961 mL | 71.7401 mL |
5 mM | 0.5739 mL | 2.8696 mL | 5.7392 mL | 14.348 mL | |
10 mM | 0.287 mL | 1.4348 mL | 2.8696 mL | 7.174 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。
TTNPB 71441-28-6 Apoptosis Autophagy Metabolism Retinoid Receptor Inhibitor Retinoic acid receptors RAR/RXR AGN191183 Arotinoid acid Ro 13-7410,AGN-191183 Ro 13-7410,AGN 191183 Retinoid X receptors Ro 13-7410,AGN191183 AGN 191183 Ro 13-7410 inhibit AGN-191183 inhibitor