Atglistatin

Atglistatin Property

Boiling point:

498.6±45.0 °C(Predicted)

Density 

1.135±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

Soluble in DMSO (up to 5 mg/ml) or in Ethanol (up to 5 mg/ml with warming)

form 

powder

pka

15.01±0.70(Predicted)

color 

white to beige

Stability:

Stable for 2 years as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

Safety

Hazard Codes 

Xn

Risk Statements 

22-36/37/38

Safety Statements 

36/37/39

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P501Dispose of contents/container to..…

Atglistatin Chemical Properties,Usage,Production

Description

Adipose triglyceride lipase (ATGL or PNPLA2) catalyzes the initial step in triglyceride hydrolysis in adipocyte and non-adipocyte lipid droplets, generating diacylglyerol. Atglistatin is a potent, selective, and competitive inhibitor of ATGL (IC₅₀ = 0.7 μM). It does not inhibit hormone-sensitive lipase, monoglyceride lipase, pancreatic lipase, lipoprotein lipase, or other lysophospholipases. Atglistatin blocks lipolysis by ATGL in vitro, in white adipose tissue organ cultures, and in vivo. It does not affect lipolysis in ATGL knockout mice.

Uses

Atglistatin has been used as a selective inhibitor of adipose triglyceride lipase (ATGL).

Biochem/physiol Actions

Atglistatin is the first selective inhibitor of adipose triglyceride lipase (ATGL), the rate limiting enzyme involved in the mobilization of fatty acids from cellular triglyceride stores. Atglistatin has an IC50 of 0.7 μM in E.coli and no activity against monoglycerol lipase (MGL), hormone-sensitive lipase (HSL), or pancreatic lipase and lipoprotein lipase PNPLA6 and PNPLA7. ATGL generates diacylglycerol from cellular triglyceride stores, which is then degraded by hormone-sensitive lipase (HSL) and monoglyceride lipase into glycerol and fatty acids, promoting the synthesis of lipotoxic metabolites that have been associated with the development of insulin resistance. Atglistatin inhibition of ATGL has been shown to reduce fatty acid mobilization in vitro and in vivo.

in vivo

References

[1] NICOLE MAYER. Development of small-molecule inhibitors targeting adipose triglyceride lipase[J]. Nature chemical biology, 2013, 9 12: 785-787. DOI:10.1038/nchembio.1359
[2] RACHID ZAGANI. Inhibition of adipose triglyceride lipase (ATGL) by the putative tumor suppressor G0S2 or a small molecule inhibitor attenuates the growth of cancer cells.[J]. Oncotarget, 2015: 28282-28295. DOI:10.18632/oncotarget.5061