Citations
3 publicationsPublications from researchers using this productDescription
C75 is a specific inhibitor of fatty acid synthase (FASN/FAS) with moderate inhibitory activity, showing an IC50 value of 15.53 μM[1]. It is used in research on obesity and cancer to explore the connection between fatty acid synthesis, energy metabolism, tumor growth, and survival. C75 is also an effective activator of CPT1A[2].
In vitro, it inhibits PC3 cell growth with a 24-hour IC50 of 35μM and reduces the growth of LNCaP spheroids in a concentration-dependent manner with an IC50 of 50μM[3]. Additionally, C75-mediated CPT 1A activation inhibits EMT, as indicated by reduced migration and α-SMA expression in HK-2 cells[4].
In vivo, C75 injection suppresses fasting-induced c-Fos expression in specific hypothalamic nuclei and reduces mouse feeding by ≥ 95% within 2 hours at a dose of 30 mg/kg[5]. In DIO mice, C75 treatment led to a 50% weight loss and a 32.9% increase in energy production due to fatty acid oxidation[2].
References:
[1] Wang X , Lin J , Chen Y ,et al.Novel fatty acid synthase (FAS) inhibitors: Design, synthesis, biological evaluation, and molecular docking studies[J].Bioorganic & Medicinal Chemistry, 2009, 17(5):1898-1904.
[2] Thupari JN, et al. C75 increases peripheral energy utilization and fatty acid oxidation in diet-induced obesity. Proc Natl Acad Sci U S A. 2002 Jul 9;99(14):9498-502.
[3] Rae C, et al. Inhibition of Fatty Acid Synthase Sensitizes Prostate Cancer Cells to Radiotherapy. RADIATION RESEARCH 184, 482–493 (2015).
[4] L Peng, C Wang, S Yu, et al. Dysregulated lipid metabolism is associated with kidney allograft fibrosis. Lipids in Health and Disease, 2024(23).
[5] Gao S, et al. Effect of the anorectic fatty acid synthase inhibitor C75 on neuronal activity in the hypothalamus and brainstem. Proc Natl Acad Sci U S A. 2003 May 13;100(10):5628-33.
Protocol
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Cell experiment [1]: |
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Cell lines |
HepG 2、SMMC 7721、Hep 3B cells |
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Preparation method |
Cells (5.0 x 106/10 cm dish) were treated with C75 for the indicated time intervals. Control cells received equivalent amounts of DMSO alone. FAS activity of cytoplasmic fractions of cells was measured by fluorescence quantification after exposure to 15 μg/ml C75 for 15 or 30 min. |
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Reaction Conditions |
15 μg/ml ; 15 or 30 min. |
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Applications |
Treatment of cells with C75 (15 μg/ml initial dose) produced significant reductions in FAS activity in HepG2 and Hep3B cells within 15 min, and in SMMC7721 cells within 30 min. |
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Animal experiment [2]: |
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Animal models |
Twelve-week-old DIO C57BL6J male mice |
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Preparation method |
DIO C57BL6J mice were fed a synthetic diet consisting of 60% calories from fat after weaning. Mice were maintained on a 12-h light-dark cycle at 25°C for 1 week before treatment. C75 and etomoxil were dissolved in RPMI medium 1640 and injected intraperitoneally at the indicated doses. Three mice were treated with C75 (20 mg/kg) on day 0. Subsequent doses were administered as follows: 15 mg/kg on day 2; 10 mg/kg on day 4; 15 mg/kg. On days 6 and 8, four mice received RPMI medium 1640. |
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Dosage form |
10-20 mg/kg; i.p. |
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Applications |
In DIO mice, C75 treatment led to a 50% weight loss and a 32.9% increase in energy production due to fatty acid oxidation |
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References: [1] Gao Y , Lin L P .Growth arrest induced by C75, A fatty acid synthase inhibitor, was partially modulated by p38 MAPK but not by p53 in human hepatocellular carcinoma.[J].Cancer Biology & Therapy, 2006, 5(8):978-985. [2] Thupari JN, et al. C75 increases peripheral energy utilization and fatty acid oxidation in diet-induced obesity. Proc Natl Acad Sci U S A. 2002 Jul 9;99(14):9498-502. |
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Product Documents
Biological Data
Chemical Properties
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
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