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C75 | MedChemExpress (MCE)

作者:MedChemExpress LLC 暂无发布时间 (访问量:227)

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C75

CAS No. : 218137-86-1

MCE 国际站:C75

产品活性:C75 是合成的脂肪酸合成酶 (FASN) 抑制剂。C75 抑制前列腺癌细胞 PC3 的 IC50 值为 35 μM。C75 是有效的 CPT1A 激活剂。

研究领域:Metabolic Enzyme/Protease

作用靶点:Fatty Acid Synthase (FASN)

In Vitro: C75 inhibits PC3 cell growht with an IC50 of 35 μM at 24 h. C75 (10-50 μM) also reduces the growth of LNCaP spheroids in a concentration-dependent manner with an IC50 of 50 μM. (-)-C75 inhibits FAS activity and has a cytotoxic effect on tumor cell lines, without affecting food consumption. (+)-C75 inhibits CPT1 and its administration produces anorexia, suggesting that central inhibition of CPT1 is essential for the anorectic effect of C75. The differential activity of C75 enantiomers may lead to the development of potential new specific drugs for cancer and obesity.

In Vivo: C75 blocks fasting-induced c-Fos expression in the arcuate nucleus (Arc), lateral hypothalamic area (LHA), and paraventricular nucleus (PVN) 10–24 h after i.p. injection. Intraperitoneal administration of C75 at 30 mg/kg body weight inhibits food intake of mice by ≥95% within 2 h after i.p. injection. C75-treated DIO mice has a 50% greater weight loss, and a 32.9% increased production of energy because of fatty acid oxidation. C75 treatment of rodent adipocytes and hepatocytes and human breast cancer cells increases fatty acid oxidation and ATP levels by increasing CPT-1 activity, even in the presence of elevated concentrations of malonyl-CoA.

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