|S4002||Sitagliptin phosphate monohydrate||41 mg/mL||100 mg/mL||<1 mg/mL|
|S3031||Linagliptin||<1 mg/mL||17 mg/mL||1 mg/mL|
|S5365||Alogliptin||18 mg/mL||67 mg/mL||67 mg/mL|
|S8565||Omarigliptin (MK-3102)||<1 mg/mL||79 mg/mL||<1 mg/mL|
|S4636||Teneligliptin hydrobromide||100 mg/mL||100 mg/mL||17 mg/mL|
|S5079||Sitagliptin||-1 mg/mL||81 mg/mL||-1 mg/mL|
Sitagliptin phosphate monohydrate is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts.
AR staining of non-CAVD and CAVD patient hVICs in the presence or absence of Sitagliptin (100 μM) after 4 weeks of osteogenic stimulation. The bar graph presents the AR-positive area measured in each culture dish.
Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9.
Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4)with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9.
Omarigliptin (MK-3102) is a competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM). It is highly selective over all proteases tested (IC50 > 67 μM), including QPP, FAP, PEP, DPP8, and DPP9 and has weak ion channel activity (IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5).
Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.
Sitagliptin is an oral and highly selective DPP-4 inhibitor with an IC50 of 18 nM. It is used for the treatment of type 2 diabetes.