2. Metabolic Enzyme/Protease
  3. FBPase
  4. 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.

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FBPase-IN-1

FBPase-IN-1 Chemische Struktur

CAS. Nr. : 20362-54-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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FBPase-IN-1 Related Antibodies

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Beschreibung

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[1].

IC50 & Target

IC50: 0.22 μM (FBPase)[1]
Cellular Effect
Cell Line Type Value Description References
HepG2 IC50
75.08 μM
Compound: 3a
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by cell counting kit-8 assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by cell counting kit-8 assay
[PMID: 32711108]
In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

FBPase-IN-1 Related Antibodies
In Vivo

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR mouse (12 h-fasted, n = 6, male)[1]
Dosage: 25 mg/kg
Administration: IP, once
Result: Lowered glucose.
Animal Model: ICR mice (6 or 7 weeks, n = 6, male)[1]
Dosage: 25 mg/kg
Administration: IP, for 4 h, once
Result: Reduced blood glucose levels by targeting FBPase and inhibiting the GNG process.
Molekulargewicht

232.37

Formel

C6H4N2S4
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

C1(SSC2=NC=CS2)=NC=CS1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Lösungsmittel & Löslichkeit
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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 8.6070 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
Verweise

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.3035 mL 21.5174 mL 43.0348 mL 107.5870 mL
5 mM 0.8607 mL 4.3035 mL 8.6070 mL 21.5174 mL
10 mM 0.4303 mL 2.1517 mL 4.3035 mL 10.7587 mL
15 mM 0.2869 mL 1.4345 mL 2.8690 mL 7.1725 mL
20 mM 0.2152 mL 1.0759 mL 2.1517 mL 5.3794 mL
25 mM 0.1721 mL 0.8607 mL 1.7214 mL 4.3035 mL
30 mM 0.1434 mL 0.7172 mL 1.4345 mL 3.5862 mL
40 mM 0.1076 mL 0.5379 mL 1.0759 mL 2.6897 mL
50 mM 0.0861 mL 0.4303 mL 0.8607 mL 2.1517 mL
60 mM 0.0717 mL 0.3586 mL 0.7172 mL 1.7931 mL
80 mM 0.0538 mL 0.2690 mL 0.5379 mL 1.3448 mL
100 mM 0.0430 mL 0.2152 mL 0.4303 mL 1.0759 mL
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FBPase-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FBPase-IN-120362-54-3FBPasefructose-1,6-bisphosphataseHepG2T2DGlucose-loweringLow toxicityInhibitorinhibitorinhibit

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