C75
目录号 : GC34065
C75是脂肪酸合成酶(FASN/FAS)的特异性抑制剂，C75显示出中等的FAS抑制活性，IC50为15.53 μM。
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.
C75是脂肪酸合成酶(FASN/FAS)的特异性抑制剂，C75显示出中等的FAS抑制活性，IC50为15.53 μM[1]。C75通常用于肥胖和癌症的研究，尤其是在探讨脂肪酸合成与能量代谢、肿瘤生长和存活之间的联系。C75也是一种有效的CPT1A激活剂[2]。
在体外，C75抑制PC3细胞生长，24h的IC50为35μM。C75 (10-50 μM) 还以浓度依赖性方式减少LNCaP球状体的生长，IC50为50μM[3]。此外，C75介导的CPT 1A激活可有效抑制EMT，表现为HK-2细胞迁移和α-SMA表达的减少[4]。
在体内，C75腹腔注射后10-24小时，阻断空腹诱导的弓状核(Arc)、下丘脑外侧区(LHA)和室旁核(PVN)中的c-Fos表达。腹膜内注射 30 mg/kg 体重的 C75 后2小时内可抑制小鼠摄食≥ 95%[5]。由于脂肪酸氧化，C75处理的DIO小鼠体重减轻了50%，能量产生增加了32.9% [2]。
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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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| Cas No. | 218137-86-1 | SDF | |
| Canonical SMILES | O=C(C(C1=C)C(CCCCCCCC)OC1=O)O | ||
| 分子式 | C14H22O4 | 分子量 | 254.32 |
| 溶解度 | DMSO : ≥ 83.3 mg/mL (327.54 mM) | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
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