C75 |
Catalog No.GC34065 |
C75 es un inhibidor de la sintasa de Ácidos grasos sintéticos (FASN); inhibe las células de cÁncer de prÓstata PC3 con un IC50 de 35 μM. C75 es un potente activador de CPT1A.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 218137-86-1
Sample solution is provided at 25 µL, 10mM.
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.
Cell experiment [1]: |
|
Cell lines |
HepG 2、SMMC 7721、Hep 3B cells |
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. |
Reaction Conditions |
15 μg/ml ; 15 or 30 min. |
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. |
Animal experiment [2]: |
|
Animal models |
Twelve-week-old DIO C57BL6J male mice |
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. |
Dosage form |
10-20 mg/kg; i.p. |
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 |
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. |
Cas No. | 218137-86-1 | SDF | |
Canonical SMILES | O=C(C(C1=C)C(CCCCCCCC)OC1=O)O | ||
Formula | C14H22O4 | M.Wt | 254.32 |
Solubility | DMSO : ≥ 83.3 mg/mL (327.54 mM) | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 3.9321 mL | 19.6603 mL | 39.3205 mL |
5 mM | 0.7864 mL | 3.9321 mL | 7.8641 mL |
10 mM | 0.3932 mL | 1.966 mL | 3.9321 mL |
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5
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