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Chemical Structure| 1469924-27-3 Chemical Structure| 1469924-27-3

Structure of Atglistatin
CAS No.: 1469924-27-3

Chemical Structure| 1469924-27-3

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Atglistatin is a potent, selective and competitive ATGL with IC50 value of 0.7 μM.

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Product Details of Atglistatin

CAS No. :1469924-27-3
Formula : C17H21N3O
M.W : 283.37
SMILES Code : O=C(NC1=CC(C2=CC=C(N(C)C)C=C2)=CC=C1)N(C)C
MDL No. :MFCD28009494
InChI Key :AWOPBSAJHCUSAS-UHFFFAOYSA-N
Pubchem ID :71699712

Safety of Atglistatin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Lipase

    ATGL, IC50:0.7 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
3T3-L1 adipocytes 0,0.1,1,10,50 μM Atglistatin inhibits lipolysis by targeting ATGL PMC3829776
HL-1 cardiomyocytes 40 mM 1 h Atglistatin significantly blocked the release of specific fatty acids that induced pro-apoptotic effects in cardiomyocytes. PMC9890462
cardiomyocytes 10 μM Atglistatin attenuated the PEDF or 44mer-induced TG lipolysis activation of cardiomyocytes. PMC4344780
3T3-L1 adipocytes 50 µM 1 hour Atglistatin effectively inhibited the release of FA from murine 3T3-L1 adipocytes by 98%. PMC5364409
SGBS adipocytes 50 µM 1 hour Atglistatin failed to inhibit FA release from SGBS adipocytes. PMC5364409

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Wild-type and ATGL-deficient (ATGL-ko) mice Oral gavage 200 μmol/kg single dose; Blood and tissues were collected after 8 hours Atglistatin showed a dose-dependent decrease in FA and glycerol levels PMC3829776
Mice catecholamine-induced cardiac damage Oral 2 mmol/kg 5 days prior to ISO application Atglistatin treatment led to a dramatic reduction of pro-fibrotic and pro-apoptotic processes, improving cardiac function. PMC9890462
Mice iCMp38αKO Oral 0.4 mg/g 2 days prior to AngII treatment and continued for 48 h thereafter Inhibition of lipolysis improved cardiac outcomes and reduced neutrophil numbers. PMC9542472
Mice Ghrelin-deficient mice Intraperitoneal injection 50 μg/g Single injection Atglistatin inhibited IGF-1-induced lipolysis in adipose tissue, blocking the increases in plasma glycerol and free fatty acids, and also blocking the increase in hepatic triglycerides, indicating that IGF-1 raises blood glucose by stimulating adipose tissue lipolysis. PMC9371671
Mice Glucocorticoid-induced metabolic syndrome model Diet 2 g/kg diet For two weeks Inhibiting lipolysis reduced glucocorticoid-induced fat mass gain, insulin resistance, and hyperglycemia PMC10300254
Mice Goat/C0//C0 mice Intraperitoneal injection 50 μg/g Single injection Atglistatin inhibited IGF-1-induced lipolysis, blocking the increase in plasma glycerol and free fatty acids, and also blocking the increase in hepatic triglycerides, thereby preventing the IGF-1-mediated increase in blood glucose. PMC9371671
Mice HFD-induced obesity model Oral 2 mmol/kg diet daily for 50 days Atglistatin effectively reduces adipose tissue lipolysis, weight gain, IR and NAFLD in mice fed a high-fat diet. PMC5364409

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.53mL

0.71mL

0.35mL

17.64mL

3.53mL

1.76mL

35.29mL

7.06mL

3.53mL

References

 

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