trans-C75

trans-C75 ((±)-C75) is an enantiomer of C75. C75 is a synthetic fatty-acid synthase (FASN) inhibitor. IC50 & Target:IC50: 35 μM (PC3 cell)^[1] In Vitro: trans-C75 ((±)-C75) inhibits PC3 cell growht with an IC₅₀ of 35 μM at 24 h.
trans-C75 ((±)-C75)(10-50 μM) also reduces the growth of LNCaP spheroids in a concentration-dependent manner with an IC₅₀ of 50 μM^[1].
trans-C75 ((±)-C75) inhibits FAS activity and has a cytotoxic effect on tumor cell lines, without affecting food consumption.
trans-C75 ((±)-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^[2]. 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^[3].
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^[4].