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Fructose 1,6-bisphosphatase-1 Inhibitor

Catalog No.
C3549
FBPase-1 inhibitor
Grouped product items
SizePriceStock Qty
5mg
$123.00
In stock
10mg
$194.00
In stock
50mg
$705.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

IC50: 3.4 μM

Fructose 1,6-bisphosphatase-1 Inhibitor is a fructose 1,6-bisphosphatase-1 inhibitor.

Fructose 1,6-bisphosphatase-1 (FBPase-1), an enzyme catalyzing the conversion of fructose-1,6-bisphosphate to fructose 6-phosphate, is one of the rate-limiting steps in gluconeogenesis. Excess hepatic fructose 1,6-bisphosphatase-1 activity contributes to hyperglycemia in patients.

In vitro: In a confirmatory assay, production of fructose-6-phosphate was monitored to give 6-phosphoglucono-d-lactone. The concomitant reduction of NADP to NADPH was also monitored. Fructose 1,6-bisphosphatase-1 Inhibitor was found to exhibit similar potency in these two distinct assays of FBPase-1 activity. Moreover, the ‘coupled’ assay format produced time-resolved data that might be subjected to kinetic analysis, indicating a Ki of 1.1μM for Fructose 1,6-bisphosphatase-1 Inhibitor. Fructose 1,6-bisphosphatase-1 Inhibitor also functioned as expected in a cellular model of glucose production. In an assay, rat hepatoma cells were starved of nutrients, making them highly dependent on the processing of pyruvate and lactate. Glucose production was measured over a three-hour period and the decrease in glucose that occurs with increasing doses of Fructose 1,6-bisphosphatase-1 Inhibitor was indicative of its ability to block gluconeogenesis by inhibiting FBPase-1 [1].

In vivo: So far, there is no animal data reported.

Clinical trial: Up to now, Fructose 1,6-bisphosphatase-1 Inhibitor is still in the preclinical development stage.

Reference:
[1] C.  Lai, R. J. Gum, M. Daly, et al. Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase. Bioorganic & Medicinal Chemistry Letters 16(7), 1807-1810 (2006).

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt377.6
Cas No.883973-99-7
FormulaC13H7Cl3N2O3S
SynonymsF1,6BPase-1 Inhibitor|FBP1 Inhibitor|FBPase-1 Inhibitor
Solubility≥37.1 mg/mL in DMSO; ≥1.84 mg/mL in EtOH with ultrasonic; insoluble in H2O
Chemical Name2,​5-​dichloro-​N-​(5-​chloro-​2-​benzoxazolyl)​-benzenesulfonamide
SDFDownload SDF
Canonical SMILESClC1=CC=C2C(N=C(NS(C3=C(Cl)C=CC(Cl)=C3)(=O)=O)O2)=C1
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

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