| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
DPP4 (dipeptidyl peptidase 4) and FAP (fibroblast activation protein). Talabostat isomer mesylate is expected to bind to the active site of DPP4 and FAP, inhibiting their enzymatic activity. DPP4 inhibition leads to increased levels of active GLP-1 and other chemokines, while FAP inhibition affects tumor stroma remodeling. The isomer may have a different selectivity profile.
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| ln Vitro |
In vitro, the active Talabostat (Val-boroPro) inhibits DPP4 with IC50 in the low nanomolar range and FAP with IC50 in the low nanomolar to sub-micromolar range. The isomer is expected to show similar or distinct inhibitory activity depending on stereochemistry. It can be used to study structure-activity relationships and off-target effects. Cell-based assays measure inhibition of DPP4 activity in lysates or on the cell surface.
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| ln Vivo |
In vivo, Talabostat has shown antitumor activity in preclinical models by enhancing immune cell infiltration and activation. The isomer may have a different pharmacokinetic or pharmacodynamic profile. It can be used to explore the role of stereochemistry in the efficacy and toxicity of DPP4/FAP inhibitors for cancer immunotherapy and diabetes research.
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| Enzyme Assay |
DPP4 enzyme activity assay (non-cell-based): Recombinant human DPP4 (1-5 nM) is incubated with increasing concentrations of Talabostat isomer mesylate (0-1000 nM) in assay buffer (50 mM Tris-HCl, pH 8.0, 0.1% BSA) for 10 min at 37degC. A fluorogenic substrate (e.g., Gly-Pro-AMC, 50 uM) is added, and fluorescence (ex=380 nm, em=460 nm) is measured for 30 min. IC50 is calculated from initial rates. FAP activity can be similarly measured using a specific substrate.
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| Cell Assay |
Cellular DPP4 activity assay: DPP4-expressing cells (e.g., Caco-2 or HEK293-DPP4) are seeded in 96-well plates. Cells are treated with Talabostat isomer mesylate (0-1000 nM) for 30-60 min at 37degC. A cell-impermeable fluorogenic DPP4 substrate (e.g., H-Gly-Pro-AMC) is added, and fluorescence released into the supernatant is measured. Alternatively, cell lysates are used for total DPP4 activity. IC50 is calculated from dose-response curves.
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| Animal Protocol |
Xenograft tumor model: Immunocompetent mice are implanted with syngeneic tumor cells (e.g., B16-F10 melanoma or Colon26 carcinoma). When tumors are established, Talabostat isomer mesylate is administered orally or intraperitoneally at doses of 1-50 mg/kg, daily for 10-21 days. Tumor volume is measured. Tumor-infiltrating lymphocytes are analyzed by flow cytometry. Chemokine levels (e.g., CXCL9, CXCL10) in plasma and tumors are measured by ELISA.
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| ADME/Pharmacokinetics |
Talabostat isomer mesylate is a small molecule with moderate oral bioavailability. As a boronic acid derivative, it has a relatively short half-life (1-2 h in rodents) due to rapid clearance. The mesylate salt enhances aqueous solubility. It is typically formulated in saline or PBS for intraperitoneal injection or in aqueous vehicles for oral gavage. The isomer may have distinct PK parameters.
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| Toxicity/Toxicokinetics |
Toxicity data for the isomer are limited. The parent compound Talabostat has been studied in clinical trials and shown acceptable safety with dose-limiting toxicities including skin rash, gastrointestinal disturbances, and reversible elevation of liver enzymes. The isomer may have a different safety profile. It is intended for research use only and not for human therapy. Standard precautions should be followed.
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| Additional Infomation |
Talabostat isomer mesylate is a research-grade chemical used to study DPP4 and FAP inhibition. Talabostat (PT-100) was evaluated in clinical trials for cancer and diabetes but did not gain FDA approval. The isomer may help understand stereospecific enzyme-inhibitor interactions. For research use only. Store as powder at -20degC, protected from light and moisture.
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| Molecular Formula |
C10H23BN2O6S
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|---|---|
| Molecular Weight |
310.18
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| Related CAS # |
Talabostat mesylate;150080-09-4;Talabostat;149682-77-9
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~322.39 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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