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Cerulenin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cerulenin图片
CAS NO:17397-89-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议

产品名称
浅蓝菌素
产品介绍
Cerulenin 是一种有效的,广泛使用的天然脂肪酸合成酶 (FASN) 抑制剂。Cerulenin 是由真菌Cephalosporium caeruleus产生的。Cerulenin 抑制拓扑异构酶I催化活性并增强 SN-38 诱导的细胞凋亡。Cerulenin 具有抗真菌和抗肿瘤活性。
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
  • Antibiotics
  • Other Antibiotics
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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.4789 mL22.3944 mL44.7888 mL
5 mM0.8958 mL4.4789 mL8.9578 mL
10 mM0.4479 mL2.2394 mL4.4789 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (11.20 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.20 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (11.20 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.20 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。