Fatostatin hydrobromide(Synonyms: 125B11 hydrobromide)

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Fatostatin hydrobromide (Synonyms: 125B11 hydrobromide) 纯度: 99.61%

Fatostatin hydrobromide (125B11 hydrobromide) 是 SREBP 活化的特异性抑制剂,可抑制 SREBP-1 和 SREBP-2 的活化。Fatostatin hydrobromide 与 SCAP (SREBP裂解激活蛋白) 结合,抑制 SREBPs 的 ER-Golgi 易位。Fatostatin hydrobromide 降低了细胞中成脂基因的转录。Fatostatin hydrobromide 具有抗肿瘤作用,能降低 ob/ob 小鼠的高血糖。

Fatostatin hydrobromide(Synonyms: 125B11 hydrobromide)

Fatostatin hydrobromide Chemical Structure

CAS No. : 298197-04-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥605 In-stock
5 mg ¥550 In-stock
10 mg ¥860 In-stock
25 mg ¥1600 In-stock
50 mg ¥2700 In-stock
100 mg ¥4100 In-stock
200 mg   询价  
500 mg   询价  

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Fatostatin hydrobromide 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Anti-Obesity Compound Library
  • Lipid Metabolism Compound Library

生物活性

Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice[1][2].

体外研究
(In Vitro)

Fatostatin hydrobromide (125B11 hydrobromide) (0.1-1 μM; 3 days) inhibits the androgen-independent prostate cancer cell proliferation (IC50=0.1 μM) in an independent of the known IGF1-signaling pathway. Fatostatin hydrobromide inhibits insulin-induced adipogenesis of 3T3-L1 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: DU-145 cells
Concentration: 0.1, 1 μM
Incubation Time: 3 days
Result: Impaired the IGF1-induced growth at an IC50 of 0.1 μM.

体内研究
(In Vivo)

Fatostatin hydrobromide (125B11 hydrobromide) (30 mg/kg; 150 mL; i.p.; daily for 28 days) reduces adiposity, ameliorates fatty liver by reducing triglyceride (TG) storage, and lowers hyperglycemia in ob/ob mice[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Four-to-five-week-old homozygous male obese (ob/ob) mice (C57BL/6J)[2]
Dosage: 30 mg/kg; 150 mL
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.

分子量

375.33

Formula

C18H19BrN2S

CAS 号

298197-04-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 22.73 mg/mL (60.56 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6643 mL 13.3216 mL 26.6432 mL
5 mM 0.5329 mL 2.6643 mL 5.3286 mL
10 mM 0.2664 mL 1.3322 mL 2.6643 mL

*

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.54 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.54 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.54 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.54 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Choi Y, et al. Identification of bioactive molecules by adipogenesis profiling of organic compounds. J Biol Chem. 2003 Feb 28;278(9):7320-4.

    [2]. Kamisuki S, et al. A small molecule that blocks fat synthesis by inhibiting the activation of SREBP. Chem Biol. 2009 Aug 28;16(8):882-92.

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