1. Immunology/Inflammation
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  3. Olitigaltin

Olitigaltin  (Synonyms: TD139; GB0139)

製品番号: HY-19940 純度: 99.74%
COA 取扱説明書 Technical Support

TD139 is a synthetic galectin-3 inhibitor. TD139 has high affinity for galectin-3 with a Kd of 68 nM, a Kd of 0.22 μM for galectin-1, and a Kd of 38 μM for galectin-7.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 1450824-22-2

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 228 在庫あり
Solution
10 mM * 1 mL in DMSO USD 228 在庫あり
Solid
1 mg $80 在庫あり
5 mg $160 在庫あり
10 mg $260 在庫あり
50 mg $940 在庫あり
100 mg $1650 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 12 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Olitigaltin purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2022 Sep 17;19(1):229.

    Relative mRNA expression of pro-inflammatory cytokines in retinas of naïve and light-exposed mice treated with vehicle or Olitigaltin (TD139, 15 mg/kg; i.p.; once daily) normalized to the reference gene Atp5b. The results showed that following treatment with TD139, the expression levels of iNOS, IL-6, and CCL2—induced by light damage—were also reduced.

    Olitigaltin purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2022 Sep 17;19(1):229.

    Olitigaltin (TD139, 15 mg/kg; i.p.; once daily) reduced microglia migration in light-exposed retinas. Representative images of Iba-1+ cells in naïve and light-exposed mice treated with vehicle or TD139 at the indicated time points. Scale bar: 50 µm. ONL, outer nuclear layer and INL, inner nuclear layer.

    Olitigaltin purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2022 Sep 17;19(1):229.

    Olitigaltin (TD139, 15 mg/kg; i.p.; once daily) delayed light-induced retinal degeneration. Representative SD-OCT scans and heat maps of retinal thickness from naïve and light-exposed mice treated with vehicle or TD139. Scale bar: 200 µm.

    Olitigaltin purchased from MedChemExpress. Usage Cited in: Autophagy. 2022 May;18(5):1020-1048.  [Abstract]

    Relative fold difference in SNCA from mDA cultured media treated with Olitigaltin (TD139) (5 μM) or vehicle (0.1% DMSO) treated control after 24 h measured by ELISA. The results showed that TD139 treatment significantly reduced SNCA secretion compared to vehicle.

    Olitigaltin purchased from MedChemExpress. Usage Cited in: Autophagy. 2022 May;18(5):1020-1048.  [Abstract]

    Representative non-reducing SDS-PAGE of concentrated EVs and the corresponding lysates from mDA neurons treated with vehicle, Olitigaltin (TD139, 1 µM; 24 h), SNCA fibrils, or TD139 + SNCA fibrils.

    Galectin アイソフォーム固有の製品をすべて表示:

    • 生物活性

    • プロトコル

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    • 参考文献

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    製品説明

    TD139 is a synthetic galectin-3 inhibitor. TD139 has high affinity for galectin-3 with a Kd of 68 nM, a Kd of 0.22 μM for galectin-1, and a Kd of 38 μM for galectin-7[1].

    IC50 & Target

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

    Cellular Effect
    Cell Line Type Value Description References
    Erythrocyte IC50
    0.3 3
    Compound: 6; TD139
    Inhibition of moues Gal3-induced hemagglutination using mouse RBC incubated for overnight by hemagglutination assay
    Inhibition of moues Gal3-induced hemagglutination using mouse RBC incubated for overnight by hemagglutination assay
    [PMID: 33988358]
    Erythrocyte IC50
    0.3 3
    Compound: 6; TD139
    Inhibition of moues Gal3-induced hemagglutination using mouse RBC incubated for overnight by hemagglutination assay
    Inhibition of moues Gal3-induced hemagglutination using mouse RBC incubated for overnight by hemagglutination assay
    [PMID: 33988358]
    Monocyte IC50
    0.08 3
    Compound: 6; TD139
    Inhibition of human Gal3-induced chemotaxis using human monocyte incubated for 4 hrs by calcein-AM dye based assay
    Inhibition of human Gal3-induced chemotaxis using human monocyte incubated for 4 hrs by calcein-AM dye based assay
    [PMID: 33988358]
    Monocyte IC50
    0.08 3
    Compound: 6; TD139
    Inhibition of human Gal3-induced chemotaxis using human monocyte incubated for 4 hrs by calcein-AM dye based assay
    Inhibition of human Gal3-induced chemotaxis using human monocyte incubated for 4 hrs by calcein-AM dye based assay
    [PMID: 33988358]
    Erythrocyte IC50
    0.3 3
    Compound: 6; TD139
    Inhibition of moues Gal3-induced hemagglutination using mouse RBC incubated for overnight by hemagglutination assay
    Inhibition of moues Gal3-induced hemagglutination using mouse RBC incubated for overnight by hemagglutination assay
    [PMID: 33988358]
    Monocyte IC50
    0.08 3
    Compound: 6; TD139
    Inhibition of human Gal3-induced chemotaxis using human monocyte incubated for 4 hrs by calcein-AM dye based assay
    Inhibition of human Gal3-induced chemotaxis using human monocyte incubated for 4 hrs by calcein-AM dye based assay
    [PMID: 33988358]
    体内実験

    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.

    臨床実験
    分子量

    648.64

    分子式

    C28H30F2N6O8S

    CAS 番号
    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

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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)

    H2O : < 0.1 mg/mL (insoluble)

    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
    10 mM 0.1542 mL 0.7708 mL 1.5417 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.

    • 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)

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始)

    C1

    ×
    体積 (開始)

    V1

    =
    濃度 (終了)

    C2

    ×
    体積 (終了)

    V2

    体内:

    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:  10% HP-β-CD in Saline water

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

    • Protocol 2

      Add each solvent one by one:  45% PEG300    5% Tween-80    50% Saline

      Solubility: 10 mg/mL (15.42 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.
    純度とドキュメンテーション

    純度: 99.74%

    参考文献
    動物実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    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
    DMSO 1 mM 1.5417 mL 7.7084 mL 15.4169 mL 38.5422 mL
    5 mM 0.3083 mL 1.5417 mL 3.0834 mL 7.7084 mL
    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
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    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

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

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
    × = ×
    C1   V1   C2   V2
    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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    製品名:
    Olitigaltin
    製品番号:
    HY-19940
    数量:
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