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TTNPB

TTNPB

产品编号 T1288   CAS 71441-28-6
别名: AGN191183, Arotinoid acid, Ro 13-7410,AGN-191183, Ro 13-7410

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。

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TTNPB Chemical Structure
TTNPB, CAS 71441-28-6
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
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MG-132限时半价
产品目录号及名称: TTNPB (T1288)
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 3.5 mg/mL (10 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Pignatello MA, et al. Toxicol Appl Pharmacol. 1997, 142(2), 319-327. 2. Pignatello MA, et al. Toxicol Appl Pharmacol. 1999, 159(2), 109-116. 3. Wu K, et al. Breast Cancer Res Treat. 2006, 96(2), 147-157. 4. Louisse J, et al. Toxicol Lett. 2011, 203(1), 1-8. 5. Darro F, et al. Breast Cancer Res Treat. 1998, 51(1), 39-55.
Hesperetin Epoxomicin Ritonavir Estramustine phosphate sodium LDC000067 (20S)-Protopanaxadiol 4EGI-1 HBDDE

相关化合物库

该产品包含在如下化合物库中:
NO PAINS 化合物库 核受体化合物库 表型筛选靶点鉴定库 干细胞分化化合物库 脂代谢化合物库 经典已知活性库 神经元分化化合物库 自噬库 已知活性化合物库 代谢化合物库

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Keywords

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

 

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