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CAS No.: 191282-48-1

trans-C75 Catalog No. CSN10522

Synonyms: (±)-C75;C 75 Trans-Racemic;C75

C75 trans is the trans form of C75, which is a potent fatty-acid synthase (FASN) inhibitor with IC50 of 35.4 μM (LNCaP cell Proliferation inhibition). According to the reporter, C75 is a racemic mixture of cis and trans C75 isomers. However, for cis isomer is less soluble in aqueous solutions and the trans isomer of C75 was soluble in culture media, the trans isomer of C75 shows more activity.

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描述Fatty Acid Synthase (FAS)is a vital enzyme which catalyzes the de novo synthesis of long chain fatty acids. C75, a synthetic inhibitor of FAS, causes anorexia and profound weight loss in lean and genetically obese mice. C75 also acts as a stimulator of carnitine palmitoyltransferase-1 to induce fatty acid oxidation. C75 treatment decreased food intake, increased energy expenditure, and reduced body weight more effectively in DIO than in lean mice. Analysis of the gene expression changes in hypothalamus demonstrated that the reduced food intake in C75-treated DIO mice might be mediated by inhibition of orexigenic neuropeptide expression and induction of anorexigenic neuropeptide expression. Gene expression changes in peripheral tissues indicated that C75 increased energy expenditure by the induction of genes involved in fatty acid oxidation. C75 also inhibited the expression of genes in peripheral tissues responsible for fatty acid synthesis and accumulation. The patterns of the changes in central and peripheral gene expression that occur with C75 treatment provide mechanisms to explain the reduced food intake and increased energy expenditure observed with C75^[2].In primary cortical neurons, C75 inhibits FAS activity and stimulates carnitine palmitoyltransferase-1 (CPT-1), consistent with its effects in peripheral tissues. C75 alters neuronal ATP levels and AMP-activated protein kinase (AMPK) activity. Neuronal ATP levels are affected in a biphasic manner with C75 treatment, decreasing initially, followed by a prolonged increase above control levels. Several downstream pathways are affected by C75 treatment, including glucose metabolism and acetyl-CoA carboxylase (ACC) phosphorylation^[3].C75 elevated hypothalamic neuronal ATP levels, which may contribute to the mechanism by which C75 decreased AMPK activity. C75 reduced the levels of pAMPKalpha and phosphorylated cAMP response element-binding protein (pCREB) in the arcuate nucleus neurons of the hypothalamus, suggesting a mechanism for the reduction in NPY expression seen with C75 treatment^[4].
参考文献

[1] Kuhajda FP, Pizer ES, Li JN, Mani NS, Frehywot GL, Townsend CA. Synthesis and antitumor activity of an inhibitor of fatty acid synthase. Proc Natl Acad Sci U S A. 2000;97(7):3450-3454. doi:10.1073/pnas.050582897
[2] Yajun Tu,et al. C75 alters central and peripheral gene expression to reduce food intake and increase energy expenditure. Endocrinology. 2005 Jan;146(1):486-93.
[3] Leslie E Landree,et al. C75, a fatty acid synthase inhibitor, modulates AMP-activated protein kinase to alter neuronal energy metabolism. J Biol Chem. 2004 Jan 30;279(5):3817-27.
[4] Eun-Kyoung Kim,et al. C75, a fatty acid synthase inhibitor, reduces food intake via hypothalamic AMP-activated protein kinase. J Biol Chem. 2004 May 7;279(19):19970-6.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 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
- 1.9660 mL
- 3.9321 mL

技术信息

CAS号

191282-48-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H22O4

运输

蓝冰

分子量

254.32

别名

(±)-C75;C 75 Trans-Racemic;C75;C75 FASN inhibitor

溶解度

DMSO	48.0 mg/mL (188.7 mM)
Water	Insoluble
Ethanol	25.0 mg/mL (98.3 mM)

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