补骨脂二氢黄酮甲醚
货号：
IB2490
品牌：
Jinpan
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产品简介
| 有效期 | 2年 |
| MDL | MFCD06858307 |
| 别名 | 甲基补骨脂黄酮 |
| 英文名称 | Bavachinin |
| CAS | 19879-30-2 |
| 分子式 | C21H22O4 |
| 分子量 | 338.4 |
| 储存条件 | 2-8℃ |
| 纯度 | HPLC≥98% |
| 外观（性状） | White to off-white Powder |
| 单位 | 瓶 |
| 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]. |
| In Vivo | 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]. |
| 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 |
| 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] |
| 细胞实验 | Animal Models: Female athymic nude mice; Dosages: 5 mg/kg; Administration: i.p.[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 |
| 规格 | 5mg 10mg 20mg |
是一种新型的PPAR激动剂