Atglistatin

Catalog No.S7364 Batch:S736401

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Technical Data

Formula

C17H21N3O
Molecular Weight 283.37 CAS No. 1469924-27-3
Solubility (25°C)* In vitro DMSO 57 mg/mL (201.15 mM)
Ethanol 4 mg/mL (14.11 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description 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.
Targets
ATGL [1]
(Cell-free assay)
0.7 μM
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]

Protocol (from reference)

Kinase Assay:[1]
  • 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.
Cell Assay:[1]
  • Cell lines

    AML-12 mouse hepatocytes

  • Concentrations

    ~50 μM

  • Incubation Time

    2 hours

  • Method

    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.
Animal Study:[1]
  • Animal Models

    Mice (C57Bl/6J)

  • Dosages

    1.4 mg/mouse (oral gavage); ~400 μmol/kg (i.p.)

  • Administration

    oral gavage or i.p.

Customer Product Validation

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

Selleck's Atglistatin has been cited by 8 publications

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

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.