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Fructose 1,6-bisphosphatase-1 Inhibitor (Synonyms: F1,6BPase-1 Inhibitor|FBP1 Inhibitor|FBPase-1 Inhibitor)

Catalog No.GC16703

Fructose 1,6-bisphosphatase-1 Inhibitor (compound 1) is a allosteric inhibitor of fructose-1,6-bisphosphatase (FBPase-1).

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Fructose 1,6-bisphosphatase-1 Inhibitor Chemical Structure

Cas No.: 883973-99-7

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5mg
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10mg
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50mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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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

Cas No. 883973-99-7 SDF
Synonyms F1,6BPase-1 Inhibitor|FBP1 Inhibitor|FBPase-1 Inhibitor
Chemical Name 2,​5-​dichloro-​N-​(5-​chloro-​2-​benzoxazolyl)​-benzenesulfonamide
Canonical SMILES ClC1=CC=C2C(N=C(NS(C3=C(Cl)C=CC(Cl)=C3)(=O)=O)O2)=C1
Formula C13H7Cl3N2O3S M.Wt 377.6
Solubility ≤14mg/ml in DMSO;20mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.6483 mL 13.2415 mL 26.4831 mL
5 mM 0.5297 mL 2.6483 mL 5.2966 mL
10 mM 0.2648 mL 1.3242 mL 2.6483 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 9 reference(s) in Google Scholar.)

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