COH-SR4

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COH-SR4  纯度: 99.73%

COH-SR4 是一种 AMPK 活化剂。COH-SR4 对白血病、黑色素瘤、乳腺癌和肺癌显示出强大的抗增殖活性。COH-SR4 通过激活 AMPK 来抑制脂肪细胞分化，有望用于肥胖及代谢紊乱相关的研究。

COH-SR4

COH-SR4 Chemical Structure

CAS No. : 73439-19-7

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生物活性

COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation. COH-SR4 can be used for the research of obesity and related metabolic disorders[1].

IC50 & Target

AMPK[1]
体外研究
(In Vitro)

COH-SR4 (1-5 μM; 24 hours) results in a dose-dependent increase in the phosphorylation of AMPK and its substrate ACC in 3T3-L1 preadipocytes, as well as in cancer cells such as HL-60, HeLa, MCF-7[1].
COH-SR4 (3-5 µM; 7 days) significantly inhibits 3T3-L1 adipocyte differentiation in a dose-dependent manner[1].
COH-SR4 (1-5 μM; 24 hours) promotes cell G1 cycle arrest[1].
COH-SR4 significantly reduces intracellular lipid accumulation and downregulates the expression of key adipogenesis-related transcription factors and lipogenic proteins[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.

Western Blot Analysis[1]

Cell Line: 3T3-L1 preadipocytes, HL-60 cells, HeLa cells, MCF-7 cells
Concentration: 1 μM, 3 μM, 5 μM
Incubation Time: 24 hours
Result: Indirectly activated AMPK.

Cell Cycle Analysis[1]

Cell Line: 3T3-L1 cells
Concentration: 1 μM, 3 μM, 5 μM
Incubation Time: 24 hours
Result: Modulated the level of proteins active during S and G2 phases of the cell cycle.

体内研究
(In Vivo)

COH-SR4 (5 mg/kg; i.g.; 3x/week; for 6 weeks) reduces body weight and fat mass in high fat diet (HFD) obese mice without affecting food intake[2].
COH-SR4 improves glycemic control and dyslipidemia in HFD obese mice[2].
COH-SR4 decreases adipose tissue hypertrophy and affects circulating adipokine levels in HFD obese mice[2].
COH-SR4 prevents hepatic lipid accumulation and fatty liver in HFD obese 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: Nine-week old male C57BL/6J mice[2]
Dosage: 5 mg/kg
Administration: Oral gavage, three times a week, for 6 weeks
Result: Decreased body weight and fat mass in HFD obese mice.

分子量

350.03

Formula

C13H8Cl4N2O
CAS 号

73439-19-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (357.11 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8569 mL 14.2845 mL 28.5690 mL
5 mM 0.5714 mL 2.8569 mL 5.7138 mL
10 mM 0.2857 mL 1.4284 mL 2.8569 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。-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 (5.94 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (5.94 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    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% corn oil

    Solubility: ≥ 2.08 mg/mL (5.94 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.94 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    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玉米油中，混合均匀。

*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]. James L Figarola, et al. Small‑molecule COH-SR4 inhibits adipocyte differentiation via AMPK activation. Int J Mol Med. 2013 May;31(5):1166-76.

    [2]. James Lester Figarola, et al. COH-SR4 Reduces Body Weight, Improves Glycemic Control and Prevents Hepatic Steatosis in High Fat Diet-Induced Obese Mice. PLoS One. 2013; 8(12): e83801.

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