Amidepsine A

- Overview
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    Background
    
    Amidepsine A is a fungal metabolite isolated from the culture broth of Humicola sp FO-2942. Amidepsine A is an inhibitor of dylglycerol acyltransferase (DGAT).
    Dylglycerol acyltransferase (DGAT) has been involved in catalyzing the formation of triglycerides from diacylglycerol and Acyl-CoA. The reaction is considered the terminal and only committed step in triglyceride synthesis and is essential for the formation of adipose tissue. There are two isozymes of DGAT have been identified: DGAT1 and DGAT2. DGAT-1 deficient mice are lean and resistant to the development of diet-induced obesity or insulin resistance [1]. DGAT2-/- mice demonstrate reduced triglyceride levels and suffer from skin barrier abnormalities [2].
    FO-2942 inhibited DGAT activity with an IC50 of 10.2 μM in rat liver microsomes. FO-2942 inhibited triacylglycerol formation in Raji cells with the IC50 value of 15.5 μM [1].
    
    [1] Tomoda H, Tabata N, Ito M, et al. Amidepsines, inhibitors of diacylglycerol acyltransferase produced by Humicola sp. FO-2942[J]. The Journal of antibiotics, 1995, 48(9): 942-947.
    [2] Smith S J, Cases S, Jensen D R, et al. Obesity resistance and multiple mechanisms of triglyceride synthesis in mice lacking Dgat[J]. Nature genetics, 2000, 25(1): 87-90.
    [3] Stone S J, Myers H M, Watkins S M, et al. Lipopenia and skin barrier abnormalities in DGAT2-deficient mice[J]. Journal of Biological chemistry, 2004, 279(12): 11767-11776.
- Properties
  - Alternative Name
    
    FO-2942A; 2,4-dimethoxy-6-methyl-benzoic acid, 4-[[4-[[(1-carboxyethyl)amino]carbonyl]-3-hydroxy-5-methylphenoxy]carbonyl]-3-hydroxy-5-methylphenyl ester
    
    CAS Number
    
    169181-28-6
    
    Molecular Formula
    
    C29H29NO11
    
    Molecular Weight
    
    567.5
    
    Appearance
    
    A powder
    
    Purity
    
    Purity ≥ 95.00%
    
    Solubility
    
    Soluble in methanol
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Amidepsine A

Background

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