CAS NO: | 17397-89-6 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
生物活性 | Cerulenin, a potent, natural inhibitor offatty acid synthase(FASN), is an epoxide produced by the fungusCephalosporium caeruleus. Cerulenin inhibitstopoisomeraseI catalytic activity and augments SN-38-inducedapoptosis. Cerulenin has antifungal and antitumor activies[1][2][3][4]. | ||||||||||||||||
IC50& Target | Fatty acid synthase (FASN)[1] | ||||||||||||||||
体外研究 (In Vitro) | Cerulenin covalently binds to the catalytic site of FAS and disrupts the condensation reaction of acetyl-COA and malonyl-COA, inhibiting the biosynthesis of fatty acids and sterols in yeast. The Flavonoids quercetin and trans-Chalcone are effective againstT. rubrum, with MICs of 125 and 7.5 μg/mL for the wild-type strain (MYA3108) and of 63 and 1.9 μg/mL for the ABC transporter mutant strain (ΔTruMDR2), respectively. The MICs of the Fluconazole and Cerulenin controls are 63 and 125 μg/mL for the wild-type strain and 30 and 15 μg/mL for the mutant strain, respectively[1]. To explore the underlying mechanism of Steroidogenic acute regulatory protein (StAR)’s protective effect on endothelial dysfunction model, the inhibitor of fatty acid synthase and HMG-CoA reductase, Cerulenin (5 μg/mL) and Lovastatin, are used before palmitic acid (PA) added. The mRNA expression of IL-1β, TNFα, VCAM-1 and IL-6 are reduced while NO production is recovered with inhibitor treatment[2]. | ||||||||||||||||
体内研究 (In Vivo) | Cerulenin treatment ofob/obmice has obvious effects on body weight. With 2 days of treatment, body weight in treated mice is decreased compared to a 5.7% weight gain in the controls. With prolonged (7 days) treatment, no body weight loss is observed, but body weight gain is slowed. In all groups, 60 mg/kg of Cerulenin is more effective than 30 mg/kg in inhibiting weight gain. If given daily or every other day, ATP content are increased 58.1% and 61.5% respectively by 7-day treatment of 60 mg/kg Cerulenin. Significant ATP elevation is also observed with only 2 days of treatment with 60 mg/kg Cerulenin. In contrast, 30 mg/kg Cerulenin, given either 2 or 7 days, does not show any significant effect on cellular ATP content[3]. | ||||||||||||||||
分子量 | 223.27 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C12H17NO3 | ||||||||||||||||
CAS 号 | 17397-89-6 | ||||||||||||||||
中文名称 | 浅蓝菌素 | ||||||||||||||||
结构分类 |
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来源 | Cephalosporium caeruleus | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 100 mg/mL(447.89 mM;Need ultrasonic) 配制储备液
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