Carmofur (HCFU) 是 5-氟尿嘧啶的衍生物，是一种抗肿瘤剂。 Carmofur 是一种酸性神经酰胺酶抑制剂，对大鼠酶的 IC50 为 79 nM。 Carmofur 抑制 SARS-CoV-2 主要蛋白酶 (Mpro)。 Carmofur 在 Vero E6 细胞中抑制 SARS-CoV-2，EC50 为 24.3 μM。
| Cas No. | 61422-45-5 |
| 别名 | 卡莫氟; HCFU |
| 化学名 | 5-fluoro-N-hexyl-2,4-dioxopyrimidine-1-carboxamide |
| Canonical SMILES | CCCCCCNC(=O)N1C=C(C(=O)NC1=O)F |
| 分子式 | C11H16FN3O3 |
| 分子量 | 257.26 |
| 溶解度 | ≥ 12.2mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Carmofur is a derivative of fluorouracil, an antimetabolite used as an antineoplastic agent. Target: Nucleoside antimetabolite/analogCarmofur, which is used in the clinic to treat colorectal cancers, is a potent AC inhibitor and that this property is essential to its anti-proliferative effects. Carmofur inhibited AC activity with a median effective concentration (IC50) of 29 ± 5 nM (mean ± standard error of the mean, s.e.m.; n = 4), whereas 5-FU had no such effect (IC50>1 mM). systemic administration of carmofur (10 or 30 mg-kg-1, intraperitoneal, i.p.) to mice produced a dose-dependent inhibition of AC activity in various tissues, including lungs and brain cortex. References:
[1]. Realini, N., et al., Discovery of highly potent acid ceramidase inhibitors with in vitro tumor chemosensitizing activity. Sci Rep, 2013. 3: p. 1035. |
