7α-hydroxy-4-Cholesten-3-one
(Synonyms: 7-羟基-4-胆甾烯-3-酮) 目录号 : GC40087
7α-Hydroxy-4-cholesten-3-one是一种由胆固醇合成胆汁酸的中间体,是pregnane X receptor(PXR)激动剂。
Cas No.:3862-25-7
Sample solution is provided at 25 µL, 10mM.
7α-Hydroxy-4-cholesten-3-one is an intermediate in the synthesis of bile acids from cholesterol and is a PXR agonist [1]. PXR is a member of the nuclear receptor superfamily and plays an important role in inducing the expression of genes related to drug transport and metabolism [2]. 7α-Hydroxy-4-cholesten-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases related to defects in bile acid biosynthesis [3]. 7α-hydroxy-4-Cholesten-3-one has anti-inflammatory and antioxidant effects [4].
In vitro, 7α-Hydroxy-4-cholesten-3-one (0-15μg/mL; 8, 24 and 48h) treatment reduced the cell viability of HepG2 cells in a time- and concentration-dependent manner. At a concentration of 10μg/mL, 57% and 37% of the cells survived after 24 hours and 48 hours of treatment, respectively [5].
References:
[1] Russell DW. The enzymes, regulation, and genetics of bile acid synthesis. Annu Rev Biochem. 2003;72:137-174.
[2] Cheng J, Shah Y M, Gonzalez F J. Pregnane X receptor as a target for treatment of inflammatory bowel disorders[J]. Trends in pharmacological sciences, 2012, 33(6): 323-330.
[3] Gälman C, et al. Bile acid synthesis in humans has a rapid diurnal variation that is asynchronous with cholesterol synthesis. Gastroenterology. 2005 Nov;129(5):1445-53.
[4] Bajor A, Kilander A, Gälman C, et al. Budesonide treatment is associated with increased bile acid absorption in collagenous colitis[J]. Alimentary pharmacology & therapeutics, 2006, 24(11‐12): 1643-1649.
[5] Lin R C, Fillenwarth M J, Du X. Cytotoxic effect of 7α-hydroxy-4-cholesten-3-one on HepG2 cells: Hypothetical role of acetaldehyde-modified Δ4-3-ketosteroid-5β-reductase (the 37-kd-liver protein) in the pathogenesis of alcoholic liver injury in the rat[J]. Hepatology, 1998, 27(1): 100-107.
7α-Hydroxy-4-cholesten-3-one是一种由胆固醇合成胆汁酸的中间体,是pregnane X receptor(PXR)激动剂 [1]。PXR是核受体超家族的一员,它在诱导与药物转运和代谢相关的基因表达方面发挥着重要作用 [2]。7α-Hydroxy-4-cholesten-3-one是胆汁酸流失,肠易激综合征和其他与胆汁酸生物合成缺陷有关的疾病的生物标志物 [3]。7α-hydroxy-4-cholesten-3-one具有抗炎和抗氧化作用 [4]。
在体外,7α-Hydroxy-4-cholesten-3-one(0-15μg/mL; 8, 24和48h)处理以时间和浓度依赖性降低了HepG2细胞的细胞活力,在10μg/mL浓度下57%和37%的细胞在处理24小时和48小时后仍存活 [5]。
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells were cultured in Way-mouth’s medium containing 10% FCS. For cytotoxicity test, cells (2×105 cells/well) were seeded into plastic 24-well tissue culture plates. Cells were incubated with 1mL of the medium at 37°C in a tissue culture incubator equilibrated with 95% air and 5% CO2. Fresh culture medium was replenished daily. 7α-Hydroxy-4-cholesten-3-one and other reagents, when indicated, were added to HepG2 cells on the fourth day when cell monolayers became confluent. Control cells received DMSO (10μL/well). Concentrations of reagents, if dissolved in DMSO, were carefully adjusted so that all wells received exactly 10μL of DMSO in total. The plates were then returned to the incubator. Except for the time course studies, cell viability was tested 24 hours after incubation with test reagents. Cell viability was measured by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method. |
Reaction Conditions | 0-15μg/mL; 8, 24 and 48h |
Applications | 7α-Hydroxy-4-cholesten-3-one treatment reduced the cell viability of HepG2 cells in a time- and concentration-dependent manner. At a concentration of 10μg/mL, 57% and 37% of the cells still survived after 24 hours and 48 hours of treatment, respectively. |
References: | |
| Cas No. | 3862-25-7 | SDF | |
| 别名 | 7-羟基-4-胆甾烯-3-酮 | ||
| 化学名 | 7α-hydroxy-cholest-4-en-3-one | ||
| Canonical SMILES | O=C1CC[C@@]2(C)C(C[C@@H](O)[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])CC[C@]4([H])[C@H](C)CCCC(C)C)=C1 | ||
| 分子式 | C27H44O2 | 分子量 | 400.6 |
| 溶解度 | DMSO : 100 mg/mL (249.60 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4963 mL | 12.4813 mL | 24.9626 mL |
| 5 mM | 499.3 μL | 2.4963 mL | 4.9925 mL |
| 10 mM | 249.6 μL | 1.2481 mL | 2.4963 mL |
| 第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
| 给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
| 第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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