Atglistatin
目录号 : GC15770
Atglistatin是一种选择性脂肪甘油三酯脂肪酶（ATGL）抑制剂（IC50 = 0.7μM）。
Cas No.:1469924-27-3
Sample solution is provided at 25 µL, 10mM.
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Atglistatin is a selective adipose triglyceride lipase (ATGL) inhibitor (IC50 = 0.7μM) [1]. Atglistatin inhibits ATGL and reduces the decomposition of triglycerides, thereby affecting the release of fatty acids and energy metabolism [2]. Atglistatin is mainly used to treat myocardial damage [3].
In B16-F10, C26, CT26, LLC, and HepG2 cells, Atglistatin (40μM; 50h, 100h, 150h) treatment reduced proliferation of all cancer cells [4]. In HT29 cells, Atglistatin (40μM; 24h) inhibits the migration and growth of colon cancer cells [5]. In A549 cells, Atglistatin (50μM, 100μM; 24h) slows the growth of cancer cells [6].
In isoprenaline mouse model, Atglistatin (2mM/kg; po; 7d, 14d) exerts its cardioprotective effects by modulating fatty acid release from white adipose tissue [3]. In isoprenaline (ISO) mouse model, Atglistatin (2mM/kg; po; 7d) ameliorates ISO-induced cardiac hypertrophy and fibrosis [7]. In the myocardial infarction model, Atglistatin (100µM/kg; po; 2d) treated mice showed significant improvement in cardiac systolic pump function [8].
References:
[1]. Mayer N, Schweiger M, Romauch M, et al. Development of small-molecule inhibitors targeting adipose triglyceride lipase. Nature chemical biology. 2013 Dec; 9(12): 785-787.
[2]. Han SL, Liu Y, Limbu SM, et al. The reduction of lipid-sourced energy production caused by ATGL inhibition cannot be compensated by activation of HSL, autophagy, and utilization of other nutrients in fish. Fish Physiology and Biochemistry. 2021 Feb; 47: 173-188.
[3]. Thiele A, Luettges K, Ritter D, et al. Pharmacological inhibition of adipose tissue adipose triglyceride lipase by Atglistatin prevents catecholamine-induced myocardial damage. Cardiovascular research. 2022 Jul 1; 118(11): 2488-2505.
[4]. Xie H, Heier C, Kien B, et al. Adipose triglyceride lipase activity regulates cancer cell proliferation via AMP-kinase and mTOR signaling. Biochimica et Biophysica Acta (BBA)-Molecular and Cell Biology of Lipids. 2020 Sep 1; 1865(9): 158737.
[5]. Iftikhar R, Penrose HM, King AN, et al. Elevated ATGL in colon cancer cells and cancer stem cells promotes metabolic and tumorigenic reprogramming reinforced by obesity. Oncogenesis. 2021 Nov 29; 10(11): 82.
[6]. Zagani R, El-Assaad W, Gamache I, et al. Inhibition of adipose triglyceride lipase (ATGL) by the putative tumor suppressor G0S2 or a small molecule inhibitor attenuates the growth of cancer cells. Oncotarget. 2015 Jul 31; 6(29): 28282.
[7]. Takahara S, Ferdaoussi M, Srnic N, et al. Inhibition of ATGL in adipose tissue ameliorates isoproterenol-induced cardiac remodeling by reducing adipose tissue inflammation. American Journal of Physiology-Heart and Circulatory Physiology. 2021 Jan 1; 320(1): H432-H446.
[8]. Bottermann K, Granade ME, Oenarto V, et al. Atglistatin pretreatment preserves remote myocardium function following myocardial infarction. Journal of Cardiovascular Pharmacology and Therapeutics. 2021 May; 26(3): 289-297.
Atglistatin是一种选择性脂肪甘油三酯脂肪酶（ATGL）抑制剂（IC50 = 0.7μM） [1]。Atglistatin 抑制ATGL并减少甘油三酯的分解，从而影响脂肪酸的释放和能量代谢 [2]。Atglistatin主要用于治疗心肌损伤 [3]。
在B16-F10、C26、CT26、LLC和HepG2细胞中，Atglistatin（40μM；50h、100h、150h）处理可降低所有癌细胞的增殖 [4]。在HT29细胞中，Atglistatin（40μM；24h）可抑制结肠癌细胞的迁移和生长 [5]。在A549细胞中，Atglistatin（50μM、100μM；24h）可减缓癌细胞的生长 [6]。
在异丙肾上腺素小鼠模型中，Atglistatin（2mM/kg；po；7d、14d）通过调节白色脂肪组织脂肪酸的释放发挥其心脏保护作用 [3]。在异丙肾上腺素（ISO）小鼠模型中，Atglistatin（2mM/kg；po；7d）可改善ISO诱导的心脏肥大和纤维化 [7]。在心肌梗死模型中，Atglistatin（100µM/kg；po；2d）治疗的小鼠心脏收缩泵功能显著改善 [8]。
| Cell experiment [1]: | |
Cell lines | B16-F10, C26, CT26, LLC, and HepG2 cells |
Preparation Method | B16-F10, C26, CT26, LLC, and HepG2 cells were cultured in RPMI 1640 medium. All media were supplemented with 10% fetal bovine serum, 100IU/L penicillin, and 0.1mg/L streptomycin. Cells were treated with Atglistatin (40μM) dissolved in dimethyl sulfoxide (DMSO). |
Reaction Conditions | 40μM; 50h, 100h, 150h |
Applications | Atglistatin treatment reduced proliferation of all cancer cells. |
| Animal experiment [2]: | |
Animal models | Isoprenaline (ISO) mouse model |
Preparation Method | 6–9 weeks old male 129/Sv mice received four repetitive subcutaneous injections of ISO hydrochloride (25 mg/kg BW/day), and saline served as vehicle. Atglistatin (ATGLi) was mixed with control diet in a final concentration of 2mM/kg. Atglistatin application was started 5 days prior to first ISO injection. Mice were pair-fed depending on food intake of Atglistatin-fed mice.14 Animals were randomized by body weight into four groups (CTRL/VEH, CTRL/ISO, ATGLi/VEH, and ATGLi/ISO) and allocated to two different study protocols. For investigation of short-term treatment effects, a first subgroup of mice [n = 10 (CTRL/VEH), n = 11 (CTRL/ISO), n = 8 (ATGLi/VEH), n = 9 (ATGLi/ISO)] was sacrificed 2 days after the final ISO application. To analyse long-term treatment effects, a second group of mice [n = 7 (CTRL/VEH), n = 12 (CTRL/ISO), n = 13 (ATGLi/VEH), n = 10 (ATGLi/ISO)] was sacrificed 12 days after the last ISO injection. The blood serum and tissue samples were collected for further analysis. |
Dosage form | 2mM/kg; po; 7d, 14d |
Applications | Atglistatin exerts its cardioprotective effects by modulating fatty acid release from white adipose tissue. |
References: | |
| Cas No. | 1469924-27-3 | SDF | |
| 化学名 | 3-[3-[4-(dimethylamino)phenyl]phenyl]-1,1-dimethylurea | ||
| Canonical SMILES | CN(C)C1=CC=C(C=C1)C2=CC(=CC=C2)NC(=O)N(C)C | ||
| 分子式 | C17H21N3O | 分子量 | 283.37 |
| 溶解度 | ≥ 14.15mg/mL in DMSO | 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 | 3.529 mL | 17.6448 mL | 35.2896 mL |
| 5 mM | 0.7058 mL | 3.529 mL | 7.0579 mL |
| 10 mM | 0.3529 mL | 1.7645 mL | 3.529 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。
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