| CAS NO: | 145414-76-2 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 372.4 |
| Cas No. | 145414-76-2 |
| Formula | C21H24O6 |
| Synonyms | 6,7-DHB |
| Solubility | ≤10mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
| Chemical Name | 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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:
[1]. Bellevue, F., Woster, P., Edwards, D., He, K., & Hollenberg, P. Synthesis and biological evaluation of 6′,7′-dihydroxybergamottin (6,7-DHB), a naturally occurring inhibitor of cytochrome P450 3A4. Bioorganic & Medicinal Chemistry Letters. 1997; 7(20): 2593-2598.
[2]. Araki, N., Tsuruoka, S., Hasegawa, G., Yanagihara, H., Omasa, T., & Enosawa, S. et al. Inhibition of CYP3A4 by 6′,7′-dihydroxybergamottin in human CYP3A4 over-expressed hepG2 cells. Journal of Pharmacy and Pharmacology. 2012; 64(12): 1715-1721.
[3]. Mohri, K., & Uesawa, Y. Effects of Furanocoumarin Derivatives in Grapefruit Juice on Nifedipine Pharmacokinetics in Rats. Pharmaceutical Research, 2001;18(2):177-182.
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