产品描述: | C75 (4-Methylene-2-octyl-5-oxotetrahydrofuran-3-carboxylicacid)是一种更稳定的浅蓝菌素合成模拟物,抑制脂肪酸合酶(fatty-acid synthase, FAS/FASN),IC50为15.53 μM,在多种癌症模型中具有潜在的治疗作用。C75也是一种有效的CPT1A激活剂。 |
靶点: |
FAS/FASN:15.53 μM;FattyAcidSynthase |
体内研究: |
C75, an alpha-methylene-gamma-butyrolactone, reduces adipose tissue and fatty liver in treated DIO mice, despite high levels of malonyl-CoA |
细胞实验: |
Cell lines: PC3, UVW and LNCaP cell lines, SK-N-BE(2c) and MCF7 cells Concentrations: 35 µM Incubation Time: 24 h Method: Cells are seeded in 25 cm2 flasks at 105 cells/flask. When cultures are in exponential growth phase, medium is removed and replaced with fresh medium (including 1% or 10% serum) containing C75 (35 mM) and simultaneous administration of x-rays (2 Gy). Cells are then incubated for 24 h at 37℃ in 5% CO2. After treatment, cells are counted and seeded for clonogenic survival assay. |
动物实验: |
Animal Models: Diet-induced obese mice model Dosages: 20, 15, 10, 15, 15 mg/kg Administration: i.p. |
参考文献: |
1. Wang X,et al. Bioorg Med Chem. 2009 Mar 1;17(5):1898-904. 2. Cheng X, et al. Org Lett. 2014 Mar 7;16(5):1414-7. 3. Rae C, et al. Adv Radiat Oncol. 2020 Jun 29;5(5):994-1005. 4. Thupari JN, et al. Proc Natl Acad Sci U S A. 2002 Jul 9;99(14):9498-502. |
溶解性: |
Soluble in DMSO、Ethanol |
保存条件: |
2-8℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.932 ml |
19.66 ml |
39.321 ml |
5 mM |
0.786 ml |
3.932 ml |
7.864 ml |
10 mM |
0.393 ml |
1.966 ml |
3.932 ml |
50 mM |
0.079 ml |
0.393 ml |
0.786 ml |
|
注意: |
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