Talabostat mesylateorally active, specific inhibitor of DPP4 CAS# 150080-09-4 |
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| Cas No. | 150080-09-4 | SDF | Download SDF |
| PubChem ID | 11522448 | Appearance | Powder |
| Formula | C10H23BN2O6S | M.Wt | 310.18 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Val-boroPro; PT100 | ||
| Solubility | >11.45mg/mL in DMSO | ||
| Chemical Name | [(2R)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid;methanesulfonic acid | ||
| SMILES | CC(C)[C@H](N)C(=O)N1CCC[C@H]1B(O)O.C[S](O)(=O)=O | ||
| Standard InChIKey | OXYYOEIGQRXGPI-WSZWBAFRSA-N | ||
| Standard InChI | InChI=1S/C9H19BN2O3.CH4O3S/c1-6(2)8(11)9(13)12-5-3-4-7(12)10(14)15;1-5(2,3)4/h6-8,14-15H,3-5,11H2,1-2H3;1H3,(H,2,3,4)/t7-,8-;/m0./s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Talabostat mesylate is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM.In Vitro:Talabostat mesylate is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630/624 and the boron of talabostat[3].In Vivo:Talabostat 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, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat 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[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. References: | |||||
Talabostat mesylate Dilution Calculator
Talabostat mesylate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.2239 mL | 16.1197 mL | 32.2393 mL | 64.4787 mL | 80.5984 mL |
| 5 mM | 0.6448 mL | 3.2239 mL | 6.4479 mL | 12.8957 mL | 16.1197 mL |
| 10 mM | 0.3224 mL | 1.612 mL | 3.2239 mL | 6.4479 mL | 8.0598 mL |
| 50 mM | 0.0645 mL | 0.3224 mL | 0.6448 mL | 1.2896 mL | 1.612 mL |
| 100 mM | 0.0322 mL | 0.1612 mL | 0.3224 mL | 0.6448 mL | 0.806 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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IC50: 1 nM
Talabostat mesilate (PT-100; Val-boroPro) is an orally active, specific inhibitor of dipeptidyl peptidases for DPP4, including tumor-associated fibroblast activation protein- (FAP).
Fibroblast activation protein- (FAP), as an integral membrane serine protease and member of the post-prolyl peptidase family, closely related to dipeptidyl peptidase IV (DPPIV) and displays a DPPIV-like fold with the characteristic /-hydrolase and eightbladed -propeller domains [1].
In vitro: By the cleavage of N-terminal Xaa-Pro or Xaa-Ala residues, talabostat blocks dipeptidyl peptidases, such as fibroblast activation protein (FAP), resulting in inducing the production of cytokine and chemokine (besides specific T-cell immunity and T-cell-dependent activity). This agent may also induce the production of colony stimulating factors, for instance, granulocyte colony stimulating factor (G-CSF), resulting in the inducement of hematopoiesis. Dipeptidyl peptidases are referred to the activation of polypeptide hormones and chemokines.
Talabostat slightly lowered the growth rates of the FAP-expressing tumors but because PT-630 and LAF-237 did not, the growth blockade was likely not related to inhibit FAP or the related post-prolyl peptidase dipeptidyl peptidase IV.[1]
In vivo: So far, no study in vivo has been conducted.
Clinical trial: Clinical study has been conducted.
Reference:
[1]. Huang Y, Simms AE, Mazur A, Wang S, León NR, Jones B, Aziz N, Kelly T. Fibroblast activation protein-α promotes tumor growth and invasion of breast cancer cells through non-enzymatic functions. Clin Exp Metastasis. 2011 Aug;28(6):567-79.
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