Saxagliptin (Onglyza) is a new dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 50 nM. BI 1356 inhibited DPP-4 activity in vitro with an IC (50) of approximately 1 nM, compared with sitagliptin (19 nM), alogliptin (24 nM), saxagliptin (50 nM), and vildagliptin (62 nM). BI 1356 was a competitive inhibitor, with a K (i) of 1 nM.
|Animal models||Male 13−14 week-old ob/ob mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 60 mg/mL|
|Related DPP-4 Products|
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(MK 0431) is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts.
Saxagliptin H2O is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
Anagliptin is a potent and selective DPP-4 inhibitor(IC50= 3.8 nM); > 10 fold less potent for DPP-8 and DPP-9.
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