FGH10019
目录号 : GC31323
FGH10019是一种固醇调节元件结合蛋白(SREBP)抑制剂，IC50值为1μM。
Cas No.:1046045-61-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Five-week-old homozygous male obese (ob/ob) mice (C57BL/6J) are housed five per cage, and had ad libitum access to normal chow and water for 1 wk after their arrival. On day 1 of the experiment, the animals (10 per group) are fed normal chow (control diet) or chow that contains 200 mg/kg of analogue 24. These doses are estimated to provide approximately 0.7 mg analogue 24 per day (appr 23 mg/kg body weight per day). Daily food intake and body weight are carefully monitored and recorded between 3:00 and 5:00 p.m. Serum constituents, and TG levels in livers are determined. |
References: [1]. Kamisuki S, et al. Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins. J Med Chem. 2011 Jul 14;54(13):4923-7. | |
FGH10019 is a novel sterol regulatory element-binding protein (SREBP) inhibitor with IC50 of 1 μM.
Treatment of the CHO-K1 cells with analog FGH10019 decreases the percentage of the mature form of SREBP-2 (68 kDa) at lower concentrations than treatment with fatostatin. Densitometric analysis of the gels indicates that the IC50 of analog FGH10019 is approximately 1 μM, which is 5-10 times lower than the IC50 of fatostatin (appr 10 μM)[1].
FGH10019-treated chow is fed at a dose rate calculated to provide about 0.7 mg analog FGH10019 per day, at about 23 mg/kg body weight, to 5-wk-old male ob/ob mice weighing an average of appr 30 g. After 8 wk on the analog 24-treated chow, the mice gain 8-9 % less weight than control mice[1].
[1]. Kamisuki S, et al. Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins. J Med Chem. 2011 Jul 14;54(13):4923-7.
| Cas No. | 1046045-61-7 | SDF | |
| Canonical SMILES | CS(=O)(NC1=CC=C(C2=CSC(C3=CC(CCC)=NC=C3)=N2)C=C1)=O | ||
| 分子式 | C18H19N3O2S2 | 分子量 | 373.49 |
| 溶解度 | DMSO : ≥ 38 mg/mL (101.74 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6774 mL | 13.3872 mL | 26.7745 mL |
| 5 mM | 0.5355 mL | 2.6774 mL | 5.3549 mL |
| 10 mM | 0.2677 mL | 1.3387 mL | 2.6774 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins
Fatostatin, a recently discovered small molecule that inhibits activation of sterol regulatory element-binding protein (SREBP), blocks biosynthesis and accumulation of fat in obese mice. We synthesized and evaluated a series of fatostatin derivatives. Our structure-activity relationships led to the identification of N-(4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)methanesulfonamide (24, FGH10019) as the most potent druglike molecule among the analogues tested. Compound 24 has high aqueous solubility and membrane permeability and may serve as a seed molecule for further development.