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Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) 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. Talabostat mesylate (Val-boroPro mesylate; PT100 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. Talabostat mesylate (Val-boroPro mesylate; PT100 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.
| Molecular Weight | 310.18 |
| Formula | C10H23BN2O6S |
| CAS Number | 150080-09-4 |
| Solubility (25°C) | Water ≥ 150 mg/mL DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Dipeptidyl Peptidase Products |
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Sitagliptin phosphate (MK-0431) is a potent inhibitor of dipeptidyl peptidase-4 (DPP-4) with IC50 of 19 nM. |
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| Alogliptin
Alogliptin is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. |
| Linagliptin
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| Vildagliptin
Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity. |
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