CAS NO: | 145414-76-2 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Cas No. | 145414-76-2 |
别名 | 二羟基香柠檬素,6,7-DHB |
化学名 | 4-[[(2E)-6,7-dihydroxy-3,7-dimethyl-2-octenyl]oxy]-7H-fuoro[3,2-g][1]benzopyran-7-one |
Canonical SMILES | O=C1C=CC2=C(OC/C=C(C)/CCC(O)C(C)(O)C)C3=C(OC=C3)C=C2O1 |
分子式 | C21H24O6 |
分子量 | 372.4 |
溶解度 | ≤10mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | IC50: 25 μM 6,7-dihydroxy Bergamottin, also known as 6,7-DHB, is a potent inhibitor of cytochrome P4503A4 (CYP3A4) with an IC50 value of 25 μM. As a primary compound in grapefruit juice, 6,7-DHB is responsible for the blockade the activity of testosterone 6β-hydrolase. CYP3A4 is an important enzyme, mainly found in both the intestinal wall and liver, which oxidizes small foreign organic molecules (xenobiotics), such as toxins or drugs. In vitro: 6,7-DHB significantly blocked the testosterone 6β-hydrolase in human liver microsomes and human CYP3A4 expressed in Escherichia coli membrane in a time- and concentration-dependent manner. Furthermore, 6,7-DHB proved to be a potent NADPH- and time-dependent inhibitor of CYP3A4 [1]. 6,7-DHB concentration-dependently inhibited nifedipine (NFP) oxidation in HepG2-GS-3A4 cell, a cell line from hepatoblastoma with overexpression of human CYP3A4 [2]. In vivo: Male Wistar-ST rats were intraduodenally administered with 6,7-DHB at a dose of 3.4 mg/ml. After 4 hours, 6,7-DHB had no significant effects on the NFP plasma concentrations, suggesting that 6,7-DHB had no pharmacokinetic effect on the rats [3]. References: |