2. Metabolic Enzyme/Protease
  3. Dipeptidyl Peptidase
  4. Talabostat mesylate

Talabostat mesylate  (Synonyms: Val-boroPro mesylate; PT100 mesylate)

Cat. No.: HY-13233A Purity: 98.35%
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Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.

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

Talabostat mesylate Chemical Structure

Talabostat mesylate Chemical Structure

CAS No. : 150080-09-4

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10 mM * 1 mL in DMSO
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Customer Review

Based on 36 publication(s) in Google Scholar

Other Forms of Talabostat mesylate:

Talabostat mesylate Related Antibodies

Top Publications Citing Use of Products

35 Publications Citing Use of MCE Talabostat mesylate

WB

    Talabostat mesylate purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2018 Dec 7;293(49):18864-18878.  [Abstract]

    Lack of evidence for directly binding to NLRP1 by Talabostat. 293T-ASC-GFPNLRP1 cells are treated with 2 μM Talabostat for 16 hours and lysed by 3 rounds of freezing and thawing. 20 μL (2 μg/uL) clarified lysates are heated at a temperature gradient for 10 minutes, centrifuged at 16,000g for 10mins at room temperature.

    View All Dipeptidyl Peptidase Isoform Specific Products:

    View All Isoforms
    DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities[1][2][3].

    IC50 & Target

    DPP-4

     

    In Vitro

    By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, Talabostat mesylate (Val-boroPro mesylate) inhibits dipeptidyl peptidases, such as FAP, resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell dependent activity[3].
    Talabostat mesylate (Val-boroPro mesylate) competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site[4].

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

    Talabostat mesylate Related Antibodies
    In Vivo

    Talabostat mesylate (Val-boroPro mesylate) can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system.
    In WEHI 164 fibrosarcoma and EL4 and A20/2J lymphoma models, Talabostat mesylate (Val-boroPro mesylate) causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory.
    Talabostat mesylate (Val-boroPro mesylate) treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[4].

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

    310.18

    Formula

    C10H23BN2O6S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(C)[C@H](N)C(N1[C@H](B(O)O)CCC1)=O.CS(=O)(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 250 mg/mL (805.98 mM; Need ultrasonic)

    DMSO : ≥ 40 mg/mL (128.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.2239 mL 16.1197 mL 32.2393 mL
    5 mM 0.6448 mL 3.2239 mL 6.4479 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 (sealed storage, away from moisture). 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
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    Concentration
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    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)

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    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 (8.06 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 (8.06 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:  PBS

      Solubility: 100 mg/mL (322.39 mM); Clear solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  Saline

      Solubility: 50 mg/mL (161.20 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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation

    Purity: 98.35%

    SDS (393 KB)

    COA (253 KB) HNMR (255 KB) RP-HPLC (266 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [4]

    Mice: BLM (0.5mg/kg/day) is administered on days -7, -6, -5, -2, -1, 0 in the nostrils of male mice. Talabostat (40 µg/mouse) or vehicle (0.9% NaCl) is dosed per os twice daily from day 1-14. MRI is performed before BLM and at days 0, 7 and 14. After the last MRI acquisition, animals are euthanised and the lungs harvested for histological and quantitative real-time polymerase chain reaction (qRT-PCR) analyses[4].

    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 (sealed storage, away from moisture). 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 / H2O 1 mM 3.2239 mL 16.1197 mL 32.2393 mL 80.5984 mL
    5 mM 0.6448 mL 3.2239 mL 6.4479 mL 16.1197 mL
    10 mM 0.3224 mL 1.6120 mL 3.2239 mL 8.0598 mL
    15 mM 0.2149 mL 1.0746 mL 2.1493 mL 5.3732 mL
    20 mM 0.1612 mL 0.8060 mL 1.6120 mL 4.0299 mL
    25 mM 0.1290 mL 0.6448 mL 1.2896 mL 3.2239 mL
    30 mM 0.1075 mL 0.5373 mL 1.0746 mL 2.6866 mL
    40 mM 0.0806 mL 0.4030 mL 0.8060 mL 2.0150 mL
    50 mM 0.0645 mL 0.3224 mL 0.6448 mL 1.6120 mL
    60 mM 0.0537 mL 0.2687 mL 0.5373 mL 1.3433 mL
    80 mM 0.0403 mL 0.2015 mL 0.4030 mL 1.0075 mL
    100 mM 0.0322 mL 0.1612 mL 0.3224 mL 0.8060 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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    Talabostat mesylate Related Classifications

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    • 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:

    Talabostat150080-09-4Val-boroProPT100PT 100PT-100Dipeptidyl PeptidaseDPPInhibitorinhibitorinhibit

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