| Bioactivity | (−)-C75 is a isoform of C75 (HY-12364), which is a synthetic fatty-acid synthase (FASN) inhibitor; inhibits prostate cancer cells PC3 with an IC50 of 35 μM[1][2][3]. C75 is a potent CPT1A activator[5]. |
| Invitro | C75 抑制 PC3 细胞生长，24 小时时的 IC50 为 35 μM。C75 (10-50 μM) 还以浓度依赖性方式减少 LNCaP 球状体的生长，IC50 为 50 μM[1]。(-)-C75 抑制 FAS 活性并对肿瘤细胞系具有细胞毒性作用，而不影响食物消耗。(+)-C75 抑制 CPT1，其给药产生厌食，表明 CPT1 的中枢抑制对于 C75 的厌食作用是必不可少的。C75 对映异构体的不同活性可能会导致开发潜在的新的癌症和肥胖特异性药物[2]。 0 --> (−)-C75 相关抗体: |
| In Vivo | 腹腔注射后 10-24 小时，C75 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%[3]。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%。C75 处理啮齿动物脂肪细胞和肝细胞以及人类乳腺癌细胞可通过增加 CPT-1 活性来增加脂肪酸氧化和 ATP 水平，即使存在升高浓度的丙二酰辅酶 A 也是如此[4]。 |
| Name | (−)-C75 |
| CAS | 1234694-22-4 |
| Formula | C14H22O4 |
| Molar Mass | 254.32 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Yan Xue, et al. Inhibition of Carnitine Palmitoyltransferase 1A Aggravates Fatty Liver Graft Injury via Promoting Mitochondrial Permeability Transition. Transplantation. 2021 Mar 1;105(3):550-560. [2]. Rae C, et al. Inhibition of Fatty Acid Synthase Sensitizes Prostate Cancer Cells to Radiotherapy. [3]. Makowski K, et al. Differential pharmacologic properties of the two C75 enantiomers: (+)-C75 is a strong anorectic drug; (-)-C75 has antitumor activity. Chirality. 2013 May;25(5):281-7. [4]. 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. [5]. 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. |