1. Immunology/Inflammation
  2. Galectin
  3. Olitigaltin

Olitigaltin  (Synonyms: TD139; GB0139)

Cat. No.: HY-19940 Purity: 99.22%
COA Handling Instructions

TD139 is an inhaled galectin-3 inhibitor with a Kd of 14 nM.

For research use only. We do not sell to patients.

Olitigaltin Chemical Structure

Olitigaltin Chemical Structure

CAS No. : 1450824-22-2

Size Price Stock Quantity
1 mg USD 80 In-stock
5 mg USD 160 In-stock
10 mg USD 260 In-stock
50 mg USD 940 In-stock
100 mg USD 1650 In-stock
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Customer Review

Based on 11 publication(s) in Google Scholar

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  • Biological Activity

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  • Customer Review

Description

TD139 is an inhaled galectin-3 inhibitor with a Kd of 14 nM.

IC50 & Target

Kd: 14 nM (galectin-3)[1]

In Vitro

TD139 is a novel synthetic inhibitor of galectin-3. TD139 has high affinity for galectin-3 with a Kd of 14 nM and 10 nM for galectin-1, but low affinity for galectins 2, 4N, 4C, 7, 8N, or 9N[1].

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

In Vivo

In primary lung AECs TD139 reduces TGF-β1–induced β-catenin translocation to the nucleus, with most of the β-catenin remaining at the cell surface. TD139 blocks TGF-β1–induced β-catenin phosphorylation. A marked reduction in fibrosis and β-catenin activation accompanied by decreased galectin-3 expression is observed in the lungs of WT mice treated with TD139[1]. Pretreatment of WT C57BL/6 mice with TD139 leads to the attenuation of liver injury and milder infiltration of IFNγ- and IL-17- and -4-producing CD4(+) T cells, as well as an increase in the total number of IL-10-producing CD4(+) T cells and F4/80(+) CD206(+) alternatively activates macrophages and preventes the apoptosis of liver-infiltrating MNCs[2].

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

Molecular Weight

648.64

Formula

C28H30F2N6O8S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]([C@@H](N1N=NC(C2=CC=CC(F)=C2)=C1)[C@H]([C@@H](CO)O3)O)[C@@H]3S[C@H]4[C@@H]([C@@H](N5N=NC(C6=CC=CC(F)=C6)=C5)[C@H]([C@@H](CO)O4)O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (77.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : ≥ 3.33 mg/mL (5.13 mM)

H2O : ≥ 1 mg/mL (1.54 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5417 mL 7.7084 mL 15.4169 mL
5 mM 0.3083 mL 1.5417 mL 3.0834 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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 (3.85 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 (3.85 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  45% PEG300    5% Tween-80    50% Saline

    Solubility: 10 mg/mL (15.42 mM); Clear solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  10% HP-β-CD

    Solubility: 3.33 mg/mL (5.13 mM); Clear solution; Need ultrasonic

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).
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
Animal Administration
[2]

Mice: The susceptibility to Con A-induced hepatitis in galectin-3-deficient mice is tested and the effects of pretreatment with a selective inhibitor of Gal-3 (TD139) in wild-type(WT) C57BL/6 mice are analyzed, as evaluated by a liver enzyme test, quantitative histology, mononuclear cell (MNC) infiltration, cytokine production, intracellular staining of immune cells, and percentage of apoptotic MNCs in the liver[2].

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

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. 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
H2O / Ethanol / DMSO 1 mM 1.5417 mL 7.7084 mL 15.4169 mL 38.5422 mL
Ethanol / DMSO 5 mM 0.3083 mL 1.5417 mL 3.0834 mL 7.7084 mL
DMSO 10 mM 0.1542 mL 0.7708 mL 1.5417 mL 3.8542 mL
15 mM 0.1028 mL 0.5139 mL 1.0278 mL 2.5695 mL
20 mM 0.0771 mL 0.3854 mL 0.7708 mL 1.9271 mL
25 mM 0.0617 mL 0.3083 mL 0.6167 mL 1.5417 mL
30 mM 0.0514 mL 0.2569 mL 0.5139 mL 1.2847 mL
40 mM 0.0385 mL 0.1927 mL 0.3854 mL 0.9636 mL
50 mM 0.0308 mL 0.1542 mL 0.3083 mL 0.7708 mL
60 mM 0.0257 mL 0.1285 mL 0.2569 mL 0.6424 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Olitigaltin 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.

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Olitigaltin
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