2. Immunology/Inflammation
  3. Galectin
  4. GB2095

GB2095 is an orally active and selective galectin-3 inhibitor. GB2095 shows superior selectivity for both human (KD = 0.036 μM) and mouse galectin-3 (KD = 0.35 μM) over other galectins (such as h-Gal-1/4N/4C/8N/8C/9N/9C and m-galectin-1). GB2095 inhibits tumor growth in syngeneic mouse models of breast and melanoma cancers. GB2095 can be used for breast and melanoma cancer research.

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GB2095

GB2095 Chemical Structure

CAS No. : 2574415-75-9

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Based on 1 publication(s) in Google Scholar

GB2095 Related Antibodies

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  • Purity & Documentation

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Description

GB2095 is an orally active and selective galectin-3 inhibitor. GB2095 shows superior selectivity for both human (KD = 0.036 μM) and mouse galectin-3 (KD = 0.35 μM) over other galectins (such as h-Gal-1/4N/4C/8N/8C/9N/9C and m-galectin-1). GB2095 inhibits tumor growth in syngeneic mouse models of breast and melanoma cancers. GB2095 can be used for breast and melanoma cancer research[1].

IC50 & Target[1]

human Galectin-3

36 nM (Kd)

mouse Galectin-3

0.35 μM (Kd)

In Vitro

GB2095 displays a 14-fold selectivity for human galectin-3 over the other tested human galectins (Gal-1, -4N, -4C, -8N, -8C, -9N, -9C) on average, and shows a more pronounced (100-fold) selectivity for mouse galectin-3 over mouse galectin-1[1].
GB2095 shows high permeability and no efflux over a CACO-2 cell monolayer, alongside good hepatic stability in both humans and mice, and exhibits moderate plasma protein binding in both human and mouse plasma[1].

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

GB2095 Related Antibodies
In Vivo

GB2095 (30 mg/kg, p.o., b.i.d from day 1 to day 14 or 25) inhibits tumor growth in breast (4T1) and melanoma (B16-F10) syngeneic mice models[1].

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

Animal Model: BALB/c mice implanted with 4T1 cells into the mammary fat pad[1]
Dosage: 30 mg/kg
Administration: p.o., b.i.d from day 1 to day 25
Result: Significantly inhibited tumor growth compared to the vehicle group, with a significant reduction in tumor volume observed from day 11.
Animal Model: C57BL/6N mice implanted with B16-F10 cells into the mammary fat pad[1]
Dosage: 30 mg/kg
Administration: p.o., b.i.d from day 1 to day 14
Result: Significantly inhibited tumor growth compared to the vehicle group, with a significant reduction in tumor volume observed from day 10.
Molecular Weight

548.79

Formula

C20H17BrClF2N3O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@@H]1[C@@H](N2C=C(C3=CC(F)=C(C(F)=C3)Cl)C=N2)[C@H]([C@H](O[C@@H]1SC4=CN=CC(Br)=C4)CO)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (182.22 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 1.8222 mL 9.1110 mL 18.2219 mL
5 mM 0.3644 mL 1.8222 mL 3.6444 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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 (4.56 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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 (protect from light)

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.
Purity & Documentation
References

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 (protect from light). 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 1.8222 mL 9.1110 mL 18.2219 mL 45.5548 mL
5 mM 0.3644 mL 1.8222 mL 3.6444 mL 9.1110 mL
10 mM 0.1822 mL 0.9111 mL 1.8222 mL 4.5555 mL
15 mM 0.1215 mL 0.6074 mL 1.2148 mL 3.0370 mL
20 mM 0.0911 mL 0.4555 mL 0.9111 mL 2.2777 mL
25 mM 0.0729 mL 0.3644 mL 0.7289 mL 1.8222 mL
30 mM 0.0607 mL 0.3037 mL 0.6074 mL 1.5185 mL
40 mM 0.0456 mL 0.2278 mL 0.4555 mL 1.1389 mL
50 mM 0.0364 mL 0.1822 mL 0.3644 mL 0.9111 mL
60 mM 0.0304 mL 0.1518 mL 0.3037 mL 0.7592 mL
80 mM 0.0228 mL 0.1139 mL 0.2278 mL 0.5694 mL
100 mM 0.0182 mL 0.0911 mL 0.1822 mL 0.4555 mL
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GB2095 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:

GB20952574415-75-9GB 2095GB-2095GalectinB16-F104T1selectiveorally activeBALB/c mouseC57BL/6N mousebreastmelanomaInhibitorinhibitorinhibit

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