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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Bavachinin
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
19879-30-2
- 规格：
10mg/5mg
| 规格： | 10mg | 产品价格： | ￥790.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥590.0 |
是一种新型的PPAR激动剂
| 基本信息 | |
| CAS | No.19879-30-2 |
| 中文名称 | 补骨脂二氢黄酮DME |
| 英文名称 | Bavachinin |
| 别名 | 补骨脂二氢黄酮DME;甲基补骨脂黄酮;Bavachinin;7-O-Methylbavachin; |
| 分子式 | C21H22O4 |
| 分子量 | 338.4 |
| 溶解性 | Soluble in DMSO ≥5mg/mL |
| 纯度 | HPLC≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD06858307 |
| SMILES | O=C1C[C@@H](C2=CC=C(O)C=C2)OC3=CC(OC)=C(C/C=C(C)\C)C=C13 |
| 靶点 | PPAR |
| 通路 | Cell Cycle;DNA Damage/DNA Repair;Metabolic Enzyme&Protease |
| 背景说明 | Bavachinin是一种新型的PPAR激动剂。 |
| 生物活性 | Bavachinin (7-O-Methylbavachin) ia a novel natural pan-PPAR agonist from the fruit of the traditional Chinese glucose-lowering herb malaytea scurfpea. It shows stronger activities with PPAR-γ than with PPAR-α and PPAR-β/δ (EC50 = 0.74 μmol/l, 4.00 μmol/l and 8.07 μmol/l in 293T cells, respectively).[1-3] |
| In Vitro | Bavachinin inhibits increases in HIF-1α activity in human KB carcinoma(HeLa cellderivative)and human HOS osteosarcoma cells under hypoxia in a concentration-dependent manner，probably by enhancing the interaction between von Hippel-Lindau(VHL)and HIF-1α. Furthermore，Bavachinin decreases transcription of genes associated with angiogenesis and energy metabolism that are regulated by HIF-1，such as vascular endothelial growth factors(VEGF)，Glut1 and Hexokinase2. Bavachinin also inhibits tube formation in human umbilical vein endothelial cells(HUVECs)as well as in vitro migration of KB cells. Bavachinin inhibits nitricoxide production in macrophages activated by lipopolysaccharide[2]. |
| 细胞实验 | In db/db and DIO mice，BVC treatment ameliorates diabetes，hyperlipidaemia and BVC improves hepatotoxicity. BVC enhances glucose transport and utilisation，hepatic lipid turnover and fatty acid metabolism through PPAR networks，thereby improving insulin sensitivity，dyslipidaemia and fatty liver[1]. In vivo studies show that injecting Bavachinin thrice weekly for four weeks significantly reduces tumor volume and CD31 expression in nude mice with KB xenografts[2]. Following IV administration of bavachinin at 25 mg/kg to na ve female BALB/c mice，clearance is high(mean CL = 299.72 mL/min/kg)and is approximately 3.33-fold of hepatic blood flow. The mean volume of distribution of bavachinin is 11881.67 mL/kg，it is 16.39 times of total body water volume(725 mL/kg)，indicating high extravascular distribution. The mean terminal half-life following IV dosing is 0.70 h，this is reflected a tight correlation between the clearance and terminal half-life. The PK properties of bavachinin are characterized as rapid oral absorption，high clearance，and poor absolute bioavailability following single oral and intravenous administration to na ve female BALB/c mice[3]. |
| 细胞实验 | Animal Models: Female athymic nude mice; Dosages: 5 mg/kg; Administration: i.p.[2] |
| 动物实验 | HOS and KB Cells(1×104)are seeded onto a 96-well plate with medium supplemented with 10% FBS and incubated for 24 h. Cells are then exposed to various concentrations of Bavachinin for an additional 24 h in hypoxic conditions. Cells are washed twice with phosphate-buffered saline and cell survival is assayed by treating with 100 μg/ml of MTT for 2h at 37 ℃. After washing with phosphate buffered saline，the resulting purple formazan is dissolved in 200 ml of dimethylsulphoxide and its absorbance is read at 540 nm.[2] |
| 数据来源文献 | [1] Feng L， et al. Diabetologia. 2016， 59(6):1276-86. [2] Nepal M， et al. Eur J Pharmacol. 2012， 691(1-3):28-37. [3] Liu L， et al. J Chromatogr B Analyt Technol Biomed Life Sci. 20 |
| 单位 | 瓶 |
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基因调控，但却有相关性。可能永生性是细胞恶变的阶段。至少在体外是如此。 （四）浸润性 浸润性是肿瘤细胞扩张性增殖行为，培养癌细胞仍持有这种性状。在与正常组织混合培养时，能浸润入其它组织细胞中，并有穿透人工隔膜生长的能力。 (T:] L(T4I tr \ （五）异质性 分学, 论坛, 化学分析, 仪器分析, 分析测试, 色谱, 电泳, 光谱:a ib m r {[1] D m T"k 所有肿瘤都是由有增殖
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IB2490 补骨脂二氢黄酮DME 细胞周期 索莱宝
￥590 - 790
