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Amidepsine D DGAT inhibitor

Catalog No.C4875
Size Price Stock Qty
1mg
$263.00
In stock
2.5 mg
$526.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & MSDS

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Chemical structure

Amidepsine D

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Chemical Properties

Cas No. 79786-34-8 SDF Download SDF
Synonyms N/A
Chemical Name 4-[(2,4-dimethoxy-6-methylbenzoyl)oxy]-2-hydroxy-6-methyl-benzoic acid, 4-carboxy-3-hydroxy-5-methylphenyl ester
Canonical SMILES OC1=C(C(O)=O)C(C)=CC(OC(C2=C(O)C=C(OC(C3=C(C)C=C(OC)C=C3OC)=O)C=C2C)=O)=C1
Formula C26H24O10 M.Wt 496.5
Solubility Soluble in DMSO Storage Store at -20°C
Physical Appearance A crystalline solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Amidepsine D 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].

References:
[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.