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FBPase-IN-1

Catalog No.GC70977

FBPase-IN-1 is a potent FBPase (Fructose-1,6-bisphosphatase) inhibitor for Type 2 diabetes (T2D) study with an IC50 of 0.22 μM.

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FBPase-IN-1 Chemical Structure

Cas No.: 20362-54-3

Size Price Stock Qty
5 mg
$135.00
In stock
10 mg
$216.00
In stock
25 mg
$410.00
In stock
50 mg
$648.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Description of FBPase-IN-1

FBPase-IN-1 is a potent FBPase (Fructose-1,6-bisphosphatase) inhibitor for Type 2 diabetes (T2D) study with an IC50 of 0.22 μM. FBPase-IN-1 can reduce blood glucose levels and ameliorate glucose tolerance. FBPase-IN-1 modifies the C128 site, regulates the N125-S124-S123 allosteric pathway of FBPase and affects the catalytic activity of FBPase.

FBPase-IN-1 (compund 3a) (1.5625-200 μM, 48 hours) shows a low cytotoxicity with an IC50 of 75.08 μM[1].
FBPase-IN-1 (0-45 min) inhibits FBPase in a time-dependent manner, with IC50 decreasing from 0.28 to 0.09 μM, shows FBPase-IN-1 is an irreversible covalent inhibitor of FBPase[1].

FBPase-IN-1 (12 h-fasted ICR mouse, n = 6, male, 25 mg/kg, IP) shows good FBPase inhibitory activity (IC50 = 0.22 μM), satisfying glucose-lowering effect in vivo (54% reduction in blood glucose at 25 mg/kg)[1].
FBPase-IN-1 (6 or 7 weeks, ICR mice, n = 6, male, 25 mg/kg, IP for 4 hours, once) reduces blood glucose levels by targeting FBPase and inhibiting the GNG process[1].

References:
[1]. Xu YX, Huang YY, Song RR, et al. Development of disulfide-derived fructose-1,6-bisphosphatase (FBPase) covalent inhibitors for the treatment of type 2 diabetes. Eur J Med Chem. 2020; 203: 112500.

Chemical Properties of FBPase-IN-1

Cas No. 20362-54-3 SDF
Formula C6H4N2S4 M.Wt 232.37
Solubility DMSO : 50 mg/mL (215.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Storage 4°C, stored under nitrogen
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 of FBPase-IN-1

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1 mg 5 mg 10 mg
1 mM 4.3035 mL 21.5174 mL 43.0348 mL
5 mM 0.8607 mL 4.3035 mL 8.607 mL
10 mM 0.4303 mL 2.1517 mL 4.3035 mL
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In vivo Formulation Calculator (Clear solution) of FBPase-IN-1

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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