Atglistatin

製品コードS7364 バッチS736402

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H21N3O
分子量 283.37 CAS No. 1469924-27-3
Solubility (25°C)* 体外 DMSO 56 mg/mL (197.62 mM)
Ethanol 12 mg/mL (42.34 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Atglistatin is a highly potent, and selective inhibitor of adipose triglyceride lipase (ATGL) with IC50 of 0.7 μM, high selectivity over other key metabolic lipases.
in vitro Atglistatin inhibits lipolysis in cell and organ cultures by targeting ATGL with no cytotoxicity up to a concentration of 50 μM. [1]
in vivo In vivo, Atglistatin (i.p.) results in Dose and time-dependent inhibition of lipolysis. Oral treatment of Atglistatin causes a dose-dependent decrease in FA and glycerol of up to 50% and 62%, respectively, and also causes a strong reduction in plasma TG levels (43%). In addition, Atglistatin shows a distinct tissue distribution and primarily accumulates in liver and adipose tissue. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Determination of lipase activity
For determination of lipase activity, lysates are incubated with a substrate containing radiolabeled [9,10-3H(N)]-triolein. Subsequently, FA are extracted and quantitated by liquid scintilation counting. Data are presented as mean ?S.D. of triplicate determinations and representative for at least three independent experiments.
細胞アッセイ 細胞株 AML-12 mouse hepatocytes
濃度 ~50 μM
反応時間 2 hours
実験の流れ For MTT-based in vitro viability assays, cells are seeded in 96-well plates and cultured under standard conditions for 24 h. The next day, cells are pretreated with different concentrations of Atglistatin dissolved in DMSO or Cisplatin dissolved in DMF as positive control for 2 h. Medium is replaced by an identical fresh medium and incubated again for the indicated time points. Thereafter, cells are incubated for 3 h with 100 μL Thiazolyl Blue Tetrazolium Bromide (MTT). The resulting violet formazan crystals are dissolved by adding 100 μL of MTT solubilization solution (0.1% NP-40, 4 mM HCl and anhydrous isopropanol). After complete dissolution of the formazan product, absorbance is measured at 595 nm using 690 nm as reference wavelength.
動物実験 動物モデル Mice (C57Bl/6J)
投薬量 1.4 mg/mouse (oral gavage); ~400 μmol/kg (i.p.)
投与方法 oral gavage or i.p.

カスタマーフィードバック

Data from [Data independently produced by , , Cancer Res, 2016, 76(5):1204-13.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Short peptides derived from pigment epithelium-derived factor attenuate retinal ischemia reperfusion injury through inhibition of apoptosis and inflammatory response in rats [ Exp Eye Res, 2024, 238:109743] PubMed: 38056550
Loss of KDM6B epigenetically confers resistance to lipotoxicity in nonalcoholic fatty liver disease-related HCC [ Hepatol Commun, 2023, 7(10)e0277] PubMed: 37782459
Loss of KDM6B epigenetically confers resistance to lipotoxicity in nonalcoholic fatty liver disease-related HCC [ Hepatol Commun, 2023, 7(10)e0277] PubMed: 37782459
Single-cell sequencing unveils key contributions of immune cell populations in cancer-associated adipose wasting [ Cell Discov, 2022, 8(1):122] PubMed: 36376273
Thioesterase superfamily member 1 undergoes stimulus-coupled conformational reorganization to regulate metabolism in mice [ Nat Commun, 2021, 12(1):3493] PubMed: 34108467
Blocking mitochondrial pyruvate import in brown adipocytes induces energy wasting via lipid cycling [ EMBO Rep, 2020, 21(12):e49634] PubMed: 33275313
Atglistatin Pretreatment Preserves Remote Myocardium Function Following Myocardial Infarction [ J Cardiovasc Pharmacol Ther, 2020, 1074248420971113] PubMed: 33150796
G0S2 Suppresses Oncogenic Transformation by Repressing a MYC-Regulated Transcriptional Program [ Cancer Res, 2016, 76(5):1204-13] PubMed: 26837760

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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