Cerulenin|17397-89-6|(浅蓝菌素)-陌孚医药/Medlife

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Cerulenin (Synonyms: 浅蓝菌素)

目录号: PC15366 纯度: ≥98%

CAS No. :17397-89-6

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中文名称	Cerulenin
中文别名	变蓝菌素;9H-嘌呤-9-乙酸,1,6-二氢-2-[(2-甲基-1-氧代丙基)氨基]-6-氧代-;浅蓝菌素;2,3-环氧-4-氧-7,10-十二碳二烯酰胺;天蓝菌素
英文名称	Cerulenin
英文别名	2-Oxiranecarboxamide,3-[(4E,7E)-1-oxo-4,7-nonadien-1-yl]-, (2R,3S)-;(2R,3S)-3-[(4E,7E)-nona-4,7-dienoyl]oxirane-2-carboxamide;Cerulenin;cerulenin (Helicocerin, NSC 116069);Cerulenin (Synthetic);2,3-Epoxy-4-oxo-7,10-dodecadienamide;caerulein A;Helicocerin;(2R,3S)-3-[(4E,7E)-1-Oxo-4,7-nonadien-1-yl]-2-oxiranecarboxamide;Crl;Nsc116069;Aids000236;Aids-000236;2,3-epoxy-4-oxo-10-dodecadienamide;CERULENIN, CEPHALOSPORIUM CAERULENS
Cas No.	17397-89-6
分子式	C₁₂H₁₇NO₃
分子量	223.27
包装储存	-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性	Cerulenin, a potent, natural inhibitor of fatty acid synthase (FASN), is an epoxide produced by the fungus Cephalosporium caeruleus. Cerulenin inhibits topoisomerase I catalytic activity and augments SN-38-induced apoptosis. Cerulenin has antifungal and antitumor activies.
性状	Solid
IC50 & Target[1][2]	Fatty acid synthase (FASN)
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 against T. 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. 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. Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Cerulenin treatment of ob/ob mice 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. Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature or refrigerated transportation.
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)
结构分类	Antibiotics Other Antibiotics
来源	Cephalosporium caeruleus
参考文献	[1]. Bitencourt TA, et al. Trans-chalcone and quercetin down-regulate fatty acid synthase gene expression and reduce ergosterol content in the human pathogenic dermatophyte Trichophyton rubrum. BMC Complement Altern Med. 2013 Sep 17;13:229. [Information] [2]. Tian D, et al. Overexpression of steroidogenic acute regulatory protein in rat aortic endothelial cells attenuates palmitic acid-induced inflammation and reduction in nitric oxide bioavailability. Cardiovasc Diabetol. 2012 Nov 21;11:144. [Information] [3]. Cheng G, et al. Cerulenin blockade of fatty acid synthase reverses hepatic steatosis in ob/ob mice. PLoS One. 2013 Sep 27;8(9):e75980. [Information] [4]. Jeong NY, et al. Fatty acid synthase inhibitor cerulenin inhibits topoisomerase I catalytic activity and augments SN-38-induced apoptosis. Apoptosis. 2013;18(2):226-237. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (447.89 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.4789 mL	22.3944 mL	44.7888 mL
5 mM	0.8958 mL	4.4789 mL	8.9578 mL
10 mM	0.4479 mL	2.2394 mL	4.4789 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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 ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 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。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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