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RGX-104 hydrochloride

RGX-104 hydrochloride

产品编号 T5128   CAS 610318-03-1
别名: SB742881, RGX-104 HCl, 盐酸RGX-104

RGX-104 hydrochloride (SB742881) 是小分子LXR 激动剂,利用 ApoE 基因的转录激活,调节先天免疫。

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RGX-104 hydrochloride Chemical Structure
RGX-104 hydrochloride, CAS 610318-03-1
规格 价格/CNY 货期 数量
1 mg ¥ 343 现货
2 mg ¥ 496 现货
5 mg ¥ 993 现货
10 mg ¥ 1,570 现货
25 mg ¥ 3,150 现货
50 mg ¥ 4,970 待询
1 mL * 10 mM (in DMSO) ¥ 1,380 现货
其他形式的 RGX-104 hydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: RGX-104 hydrochloride (T5128)
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纯度: 99.49%
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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 RGX-104 hydrochloride (SB742881) is a liver X receptor (LXR) agonist with potential immunomodulating and antineoplastic activities. It modulates innate immunity via transcriptional activation of the ApoE gene.
体内活性 Oral administration of RGX-104 to animals bearing palpable tumors significantly suppressed the growth of multiple cancer types. Strong tumor growth suppression was also observed in animals bearing large tumors. As compared to controls after 8 days of treatment, apoptotic circulating G-MDSCs of total CD45+ lymphocytes in RGX-104-treated (100 mg/kg) mice had a significant increase.
细胞实验 Myeloid-derived suppressor cells were isolated as previously described from splenic tissue of tumor-bearing mice. One hundred thousand cells were plated in quadruplicates in poly-L-lysine coated plates. After 3 hours of treatment with 1uM RGX-104 or DMSO as vehicle, cells were fixed with 4% PFA for 15 minutes and wash 3 times with 1X PBS prior staining. Rabbit monoclonal anti-Ki67 antibody (1:400 dilution) was applied at 4C overnight. Cells were incubated with Alexa Fluor 488 secondary antibody (1:200 dilution) for one hour at room temperature, counterstained with DAPI (1:1000 dilution) and mounted with Prolong Gold. For the analysis of the percentage of Ki67 positive cells, five fields from each replicate were imaged at 20x magnification using Zeiss Axio Imager fluorescence microscope.
动物实验 For MDSC adoptive transfer experiments into tumor-bearing mice, 2 × 10^6 MDSCs were isolated as described above from C57BL/6 tumor-bearing mice and subsequently labeled with BD Horizon Violet (BV) Proliferation Dye and then adoptively transferred via retro-orbital injection into wild-type mice. Mice were then treated with RGX-104 (100 mg/kg/day) or control diet for 36 hours. Spleens of recipient mice were then harvested and processed for flow cytometry analysis as described above. For MDSC adoptive transfer experiments in to WT and ApoE?/? non-tumor bearing mice, 5 × 10^6 MDSCs were isolated as described above from tumor-bearing mice (either wild-type C57BL/6 or Apoe?/? mice) and subsequently labeled with BV cell tracker dye and then adoptively transferred via retro-orbital injection into either wild-type or Apoe?/? mice. Mice were then treated with GW3965 (100 mg/kg/day) or control diet for 48 hours. Spleens of recipient mice were then harvested and processed for flow cytometry analysis.
别名 SB742881, RGX-104 HCl, 盐酸RGX-104
分子量 632.54
分子式 C34H34Cl2F3NO3
CAS No. 610318-03-1

存储

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

溶解度

DMSO: 115 mg/mL (181.81 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 1.5809 mL 7.9046 mL 15.8093 mL 39.5232 mL
5 mM 0.3162 mL 1.5809 mL 3.1619 mL 7.9046 mL
10 mM 0.1581 mL 0.7905 mL 1.5809 mL 3.9523 mL
20 mM 0.079 mL 0.3952 mL 0.7905 mL 1.9762 mL
50 mM 0.0316 mL 0.1581 mL 0.3162 mL 0.7905 mL
100 mM 0.0158 mL 0.079 mL 0.1581 mL 0.3952 mL

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TargetMol Library Books参考文献

1. Tavazoie MF, et al. LXR/ApoE Activation Restricts Innate Immune Suppression in Cancer. Cell. 2018 Feb 8;172(4):825-840.e18.
Icariside E4 GSK3987 AZ876 GAC0003A4 Saikosaponin A T0901317 Licochalcone E BMS-779788

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌活性化合物库 药物功能重定位化合物库 抗癌药物库 代谢化合物库 口服活性化合物库 抗癌化合物库 血液病分子库 已知活性化合物库 经典已知活性库

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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。

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Keywords

RGX-104 hydrochloride 610318-03-1 Metabolism Liver X Receptor RGX 104 Hydrochloride inhibit LXR RGX-104 RGX 104 RGX104 Hydrochloride SB742881 SB-742881 RGX-104 Hydrochloride RGX 104 hydrochloride RGX-104 HCl RGX104 hydrochloride Inhibitor SB 742881 盐酸RGX-104 RGX104 Liver X receptor inhibitor

 

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