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A939572 Stearoyl-CoA desaturase1 (SCD1) inhibitor

Catalog No.B3607
Size Price Stock Qty
10mM (in 1mL DMSO)
$210.00
In stock
10mg
$100.00
In stock
50mg
$425.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

A939572

Protocol

Animal experiment [1]:

Animal models

ob/ob mice

Dosage form

10 mg/kg; b.i.d.

Applications

In ob/ob mice, A939572 lowered the desaturation index (18:0/18:1n9). Moreover, A939572 reduced triglyceride desaturation index in a dose-dependent manner.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Xin Z, Zhao H, Serby M D, et al. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorganic & medicinal chemistry letters, 2008, 18(15): 4298-4302.

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Chemical Properties

Cas No. 1032229-33-6 SDF Download SDF
Chemical Name 4-(2-chlorophenoxy)-N-(3-(methylcarbamoyl)phenyl)piperidine-1-carboxamide
Canonical SMILES CNC(C1=CC(NC(N2CCC(OC3=CC=CC=C3Cl)CC2)=O)=CC=C1)=O
Formula C20H22ClN3O3 M.Wt 387.86
Solubility >17.15mg/mL in DMSO Storage Store at -20°C
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

A939572 is a potent and orally bioavailable inhibitor of stearoyl-CoA desaturase1 (SCD1) with IC50 value of 37nM [1].

SCD is a microsomal enzyme that catalyzes the biosynthesis of monounsaturated fatty acids. One member of SCD family, SCD1, is regulated by dietary and hormonal factors and is proved to play an important role in lipid metabolism and body weight control. Thus, SCD1 is a target for the treatment of obesity and diabetes. A939572 is a synthetic inhibitor of SCD1 with improved inhibitory activity and lipophilicity than its parent compound. It shows inhibition of mouse SCD1 and human SCD1 with IC50 values of <4nM and 37nM, respectively. In addition, A939572 has no inhibitory activity to the co-enzymes of SCD1, cytochrome b5 and cytochrome b5 reductase. It suggests that A939572 interacts with SCD1 directly and specifically. Furthermore, A939572 shows high oral bioavailability in mice [1].

References:
[1] Xin Z, Zhao H, Serby M D, et al. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorganic & medicinal chemistry letters, 2008, 18(15): 4298-4302.