浅蓝菌素作用机制 - Medchemexpress - MCE中国

Product Data?SheetCeruleninCat. No.:CAS No.:分?式:分?量:作?靶点:作?通路:储存?式:HY-A021017397-89-6C??H??NO?223.27Fatty Acid Synthase (FAS); FungalMetabolic Enzyme/Protease; Anti-infectionPowderIn solvent-20°C-80°C-20°C3 years6 months1 monthInhibitors?Agonists?Screening Libraries溶解性数据体外实验DMSO : 100 mg/mL (447.89 mM; Need ultrasonic)Mass1 mg5 mg10 mgSolventConcentration制备储备液1 mM5 mM10 mM4.4789 mL0.8958 mL0.4479 mL22.3944 mL4.4789 mL2.2394 mL44.7888 mL8.9578 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；?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?式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个?内使?，-20°C 储存时，请在 1 个?内使?。体内实验请根据您的实验动物和给药?式选择适当的溶解?案。以下溶解?案都请先按照 In Vitro ?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?作液，建议您现?现配，当天使?； 以下溶剂前显?的百分?是指该溶剂在您配制终溶液中的体积占?；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?式助溶1. 请依序添加每种溶剂：?10% DMSO ?? 40% PEG300 ?? 5% Tween-80 ?? 45% salineSolubility: ≥ 2.5 mg/mL (11.20 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (11.20 mM，饱和度未知) 的澄清溶液。 以 1 mL ?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? 50 μL Tween-80，混合均匀；然后继续加? 450 μL ?理盐?定容? 1 mL。2. 请依序添加每种溶剂：?10% DMSO ?? 90% corn oilSolubility: ≥ 2.5 mg/mL (11.20 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (11.20 mM，饱和度未知) 的澄清溶液，此?案不适?于实验周期在半个?以上的实验。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ??油中，混合均匀。Page 1 of 2 www.MedChemExpress.cn

BIOLOGICAL ACTIVITY?物活性Cerulenin 是?种?泛使?的天然脂肪酸合成酶 (FAS) 抑制剂。Cerulenin 是由真菌 Cephalosporium caeruleus 产?的。IC?? & Target体外研究Fatty acid synthase (FAS)[1]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[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[3].PROTOCOLCell Assay [2]Rat aortic endothelial cells (RAECs) are isolated and cultured with minor modifications. Briefly, segments of thoracic aorta are excised from male Wistar rats (150-180 g) and immediately placed in cold PBS containing 100 U/mL Penicillin and 100 mg/mL Streptomycin. The aorta is cut into 1 millimeter wide rings after the periadventitial fat is removed. Following transferred to a T-25 cm2 flasks, the rings are cultured in Medium 199 containing 20% fetal bovine serum, 2.5 ng/mL basic fibroblast growth factors, 100U/mL Penicillin and 100 mg/mL Streptomycin. The aorta rings are placed at 37°C in a humidified atmosphere with 5% CO2 for 72-80 h without movement. All pieces of aorta rings are removed when cells migrated. Its microvascular cytological characteristics are demonstrated by CD31 and vWF staining. In experiments involving PA treatment, M199 medium supplemented with 1% bovine serum albumin is used. All experiments are performed with RAECs up to passage 4. In the experiments with inhibitor, 5 μg/mL Cerulenin (in ethonal), or 5 μM Lovastatin (in DMSO), or 3.3 μg/mL Cerulenin plus 3.3 μM Lovastatin is added in culture media 24 hours prior to PA treatment. The same volume of solvents is added at the same time as control[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Administration [3]mice[3] Cerulenin is given to 6-8 week old male ob/ob mice in RPMI medium containing 20% DMSO intraperitoneally (i.p.). Controls are injected similarly with vehicle alone. The experimental groups (4 mice each) are as follows: A: 60 mg/kg/day Cerulenin, injected daily for 7 days; B: 60 mg/kg every other day for 7 days; C: 30 mg/kg/day for 7 days; D: 30 mg/kg every other day for 7 days; E: vehicle, daily for 7 days; F: 60 mg/kg/day Cerulenin for 2 days; G: 30 mg/kg/day Cerulenin for 2 days; H: vehicle, daily for 2 days; I: control. All animals are sacrificed on the same day under anesthesia. Blood is collected by portal vein puncture. Liver samples are snap-frozen in liquid N2 and stored at -80°C until analysis, or paraformaldehyde-fixed for histological analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3

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????J Hepatol. 2024 May;72(5):976-989.????Cell Death Dis. 2024 May 2;9(5):505.

See more customer validations on www.MedChemExpress.cnREFERENCES

[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.

[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.

[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.

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