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

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

Cat. No.: HY-13233A Purity: >98.0%
Handling Instructions

Talabostat mesylate (Val-boroPro mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical 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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 192 In-stock
Estimated Time of Arrival: December 31
50 mg USD 490 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Talabostat mesylate:

Top Publications Citing Use of Products

    Talabostat mesylate purchased from MCE. Usage Cited in: bioRxiv. Feb. 7, 2018.

    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.
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    Description

    Talabostat mesylate (Val-boroPro mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical 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

    IC50: < 4 nM (DPP-IV), 4/11 nM (DPP8/9), 310 nM (QPP), 560 nM (FAP)[1]
    Ki: 0.18 nM (DPP-IV), 1.5/0.76 nM (DPP8/9)[2]

    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].

    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].

    Clinical Trial
    Molecular Weight

    310.18

    Formula

    C₁₀H₂₃BN₂O₆S

    CAS No.

    150080-09-4

    SMILES

    CC(C)[[email protected]](N)C(N1[[email protected]](B(O)O)CCC1)=O.CS(=O)(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 : ≥ 40 mg/mL (128.96 mM)

    *"≥" 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
    10 mM 0.3224 mL 1.6120 mL 3.2239 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (8.06 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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
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    Product Name:
    Talabostat mesylate
    Cat. No.:
    HY-13233A
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