Bergapten

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

5-甲氧基补骨脂素是一种天然存在的线性呋喃香豆素，已成功与紫外线 (UV) A 照射[补骨脂素加紫外线 (PUVA)] 结合使用来治疗牛皮癣和白癜风。

5-Methoxypsoralen, a naturally occurring linear furocoumarin, has been successfully used in combination with ultraviolet (UV) A irradiation [psoralen plus UV (PUVA)] to manage psoriasis and vitiligo; inhibit proliferation in the human hepatocellular carcinoma cell line.(In Vitro):There is decreased N-acetyltransferase (NAT) activity in SC-M1 cells at concentrations of Bergapten (5-Methoxypsoralen, 5-MOP) from 0.05 mM to 25 mM, but no obvious dose-dependent effect is found between these doses (r=0.5687). In COLO 205 cells, there is decreased NAT activity at low doses of Bergapten (0.05 mM and 0.5 mM) and increased NAT activity at a high dose (50 mM). Bergapten induces a dosedependent effect in our experimental concentrations on COLO 205 cells (r=0.8912); a promotion effect at a higher dose (50 mM) and an inhibition effect at lower doses (0.05-0.5 mM), while the concentrations 5-25 mM has no significant difference compared with the control regimen. Bergapten (5-Methoxypsoralen) exerts inhibitory effects on diabetes-related osteoporosis via the regulation of the PI3K/AKT, JNK/MAPK and NF-κB signaling pathways in osteoprotegerin knockout mice. Bergapten has also been shown to significantly inhibit the production of pro-inflammatory cytokines. Bergapten exhibits the ability to significantly inhibit RANKL-RANK signaling transduction, and to suppress the activation of the PI3K/AKT, JNK/MAPK and NF-κB signaling pathways, thus protecting trabecular structure and decreasing osteoclastogenic differentiation. (In Vivo):The metabolic activity of NAT of the rat colon is higher than that of the stomach, and Bergapten (5-Methoxypsoralen, 5-MOP) causes a decrease of AF concentration in the stomach at the 24-h time-period. The concentrations of AAF in the stomach and colon are low. Although DMSO (solvent) influenced the metabolism of AAF, compared with the control regimen, Bergapten still causes an increase in the further metabolism of AAF, and a decrease in the concentration of AAF in the stomach at 24 h, and in the colon during the 24- to 72-h time-period.

There is decreased N-acetyltransferase (NAT) activity in SC-M1 cells at concentrations of Bergapten (5-Methoxypsoralen, 5-MOP) from 0.05 mM to 25 mM, but no obvious dose-dependent effect is found between these doses (r=0.5687). In COLO 205 cells, there is decreased NAT activity at low doses of Bergapten (0.05 mM and 0.5 mM) and increased NAT activity at a high dose (50 mM). Bergapten induces a dosedependent effect in our experimental concentrations on COLO 205 cells (r=0.8912); a promotion effect at a higher dose (50 mM) and an inhibition effect at lower doses (0.05-0.5 mM), while the concentrations 5-25 mM has no significant difference compared with the control regimen. Bergapten (5-Methoxypsoralen) exerts inhibitory effects on diabetes-related osteoporosis via the regulation of the PI3K/AKT, JNK/MAPK and NF-κB signaling pathways in osteoprotegerin knockout mice. Bergapten has also been shown to significantly inhibit the production of pro-inflammatory cytokines. Bergapten exhibits the ability to significantly inhibit RANKL-RANK signaling transduction, and to suppress the activation of the PI3K/AKT, JNK/MAPK and NF-κB signaling pathways, thus protecting trabecular structure and decreasing osteoclastogenic differentiation.

The metabolic activity of NAT of the rat colon is higher than that of the stomach, and Bergapten (5-Methoxypsoralen, 5-MOP) causes a decrease of AF concentration in the stomach at the 24-h time-period. The concentrations of AAF in the stomach and colon are low. Although DMSO (solvent) influenced the metabolism of AAF, compared with the control regimen, Bergapten still causes an increase in the further metabolism of AAF, and a decrease in the concentration of AAF in the stomach at 24 h, and in the colon during the 24- to 72-h time-period.

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Metabolic Enzyme/Protease

P450

CYP

Cancer

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484-20-8

216.19

C12H8O4

>98% (HPLC)

DMSO: 5 mg/mL (23.12 mM)

COC1=C2C=CC(=O)OC2=CC2=C1C=CO2

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(-20℃)

With Ice Pack

≥ 2 years