异水飞蓟宾 T3797
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
100 mg | 72581-71-6 | ¥5,120.00 | 询底价 |
1 mg | 72581-71-6 | ¥247.00 | 询底价 |
5 mg | 72581-71-6 | ¥690.00 | 询底价 |
10 mg | 72581-71-6 | ¥995.00 | 询底价 |
50 mg | 72581-71-6 | ¥3,530.00 | 询底价 |
25 mg | 72581-71-6 | ¥2,320.00 | 询底价 |
1 mL | 72581-71-6 | ¥748.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Isosilybin
描述: Isosilybin (Isosilibinin) 是一种类黄酮,来源于乳蓟;能够抑制CYP3A4诱导(IC50:74 μM)。
细胞实验: LNCaP cells and 22Rv1 cells are plated and treated at 40–50% confluency with different doses of isosilybin B and isosilybin A (10–90 μM in medium) dissolved originally in Dimethyl sulfoxide (DMSO) for the desired time periods (24–48 h) in serum condition. An equal amount of DMSO (vehicle) is present in each treatment, including control; DMSO concentration did not exceed 0.1% (v/v) in any treatment. At the end of desired treatments, total cell number is determined by counting each sample in duplicate using a hemocytometer under an inverted microscope. Cell viability is determined using trypan blue exclusion method[2].
体外活性: 报告基因检测表明,奶蓟的成分silybin和isosilybin负责抑制奶蓟对PXR介导的CYP3A4诱导的抑制作用。与silybin相比,异构体isosilybin对PXR介导的CYP3A4诱导具有更强的抑制作用。89, 133和200 μM的isosilybin溶液分别可以显著抑制CYP3A4诱导64, 82和88%。isosilybin以IC50 为74 μM抑制CYP3A4诱导[1]。从水飞蓟中分离的两种对映异构体isosilybin B和isosilybin A具有通过细胞周期阻滞和诱导凋亡介导的抗前列腺癌(PCA)活性。isosilybin B和isosilybin A处理导致人类前列腺癌LNCaP和22Rv1细胞的生长抑制和细胞死亡,伴随着强烈的G(1)期阻滞和凋亡[2]。isosilybin B导致Akt(Ser-473和Thr-308)和Mdm2(Ser-166)的磷酸化增强,这与雄激素受体降解有关,以PI3K抑制剂(LY294002)预处理恢复雄激素受体水平。isosilybin B处理促进了Akt、Mdm2和AR之间复合物的形成,这促进了依赖磷酸化的AR泛素化及其通过蛋白酶体的降解[3]。在30 μM浓度下,isosilybin A能显著激活PPARγ(2.08±0.48倍,p<0.01)。isosilybin A引起PPARγ依赖性萤光素酶报告基因的浓度依赖性转录激活。体内模拟对接研究表明,与无活性的水飞蓟成分相比,3的结合模式不同,它在受体配体结合域的入口区域额外形成一个与Ser342的氢键[4]。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 88 mg/mL(182.4 mM)
Chloroform, Dichloromethane, Ethyl Acetate : Soluble
关键字: Cytochrome P450 | Inhibitor | Q 100795 | Isosilybin | inhibit | CYPs | Q100795
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途