FATOSTATIN A
| 中文名称 | FATOSTATIN A |
|---|---|
| 中文同义词 | 脂肪抑制素;2-(2-丙基吡啶-4-基)-4-(对甲苯基)噻唑;化合物FATOSTATIN A;FATOSTATIN FREE BASE |
| 英文名称 | Fatostatin A |
| 英文同义词 | 4-(4-methylphenyl)-2-(2-propylpyridin-4-yl)-1,3-thiazole;125B11;Pyridine, 4-[4-(4-methylphenyl)-2-thiazolyl]-2-propyl-;2-(2-propylpyridin-4-yl)-4-(p-tolyl)thiazole;mice,125B11,prostate,cancer,Fatty Acid Synthase (FASN),gene,human,insulin-induced,Fatostatin,ob/ob,inhibit,expression,Golgi,Inhibitor,adipogenesis,SREBP-mediated |
| CAS号 | 125256-00-0 |
| 分子式 | C18H18N2S |
| 分子量 | 294.41 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 125256-00-0.mol |
| 结构式 |  |
FATOSTATIN A 性质
| 沸点 | 474.3±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.125±0.06 g/cm3(Predicted) |
| 储存条件 | under inert gas (nitrogen or Argon) at 2-8°C |
| 溶解度 | 溶于 DMSO（高达 25 mg/ml）。 |
| 形态 | 固体 |
| 酸度系数(pKa) | 3.46±0.10(Predicted) |
| 颜色 | 粘黄色 |
| 稳定性 | DMSO中的溶液可在-20°下稳定储存3个月。 |
Fatostatin (125B11) 是一种diarylthiazole的衍生物，是 Sterol regulatory element binding proteins (SREBPs) 活化的特异性抑制剂。Fatostatin 可结合SCAP (SREBP cleavage-activating protein)，并抑制SREBP的ER-Golgi易位。Fatostatin 可抑制癌细胞生长并增强癌细胞的凋亡。
| Target | Value |
|
SREBP
() |
Fatostatin (125B11) (0.1-1 μM; 3 days) inhibits the androgen-independent prostate cancer cell proliferation (IC
50
=0.1 μM) in an independent of the known IGF1-signaling pathway. Fatostatin inhibits insulin-induced adipogenesis of 3T3-L1 cells.
Fatostatin directly binds SCAP and blocks its ER-to-Golgi transport with IC
50
of 2.5 and 10 μM in mammalian cells.
Cell Proliferation Assay
| Cell Line: | DU-145 cells |
| Concentration: | 0.1, 1 μM |
| Incubation Time: | 3 days |
| Result: | Impaired the IGF1-induced growth at an IC 50 of 0.1 μM. |
Fatostatin (125B11) (30 mg/kg; 150 μL; i.p. injection; daily for 28 days) reduces adiposity, ameliorated fatty liver by reducing triglyceride (TG) storage, and lowered hyperglycemia in ob/ob mice.
| Animal Model: | Four-to-five-week-old homozygous male obese ( ob/ob ) mice (C57BL/6J) |
| Dosage: | 30 mg/kg; 150 μL |
| Administration: | i.p. injection; daily for 28 days |
| Result: | Blocked increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice, even under uncontrolled food intake. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/16 | S9785 | FATOSTATIN A Fatostatin | 125256-00-0 | 5mg | 795.2元 |
| 2024/01/16 | S9785 | Fatostatin | 125256-00-0 | 10mM (1mL in DMSO) | 958.23元 |