Vildagliptin (LAF-237) 274901-16-5

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Molecular Weight:

303.4 Vildagliptin (LAF-237) inhibits DPP−4 with IC50 of 2.3 nM.






Biological Activity


Vildagliptin is the most stable DPP-IV inhibitor, binding in the S1- and
S2-catalytic sites of DPP-IV, possessing a P-1 site transition-state
mimetic.


Vildagliptin(orally dosed with 10 μmol/kg) is a potent, orally active
inhibitor of plasma DPP-IV activity that provides increased levels of
GLP-1 in an oral glucose tolerance test (OGTT) with Obese male Zucker
rats.


Vildagliptin orally dosed with 10 μmol/kg both significantly
decreases glucose excursions and stimulates insulin secretion in Obese
male Zucker rats. Maximum inhibition of plasma DPP-IV activity (95%) is
observed approximately 2 hours postdose of Vildagliptin (1 μmol/kg, po)
while >50% inhibition of DPP-IV is observed within 30 min postdose
and persisted for >10 hours in normal Cynomolgus monkeys.


Vildagliptin(60 mg/kg) increases pancreatic beta cell mass through
enhanced beta cell replication and reduced Apoptosis, and the increased
beta cell mass is sustained for 12 days after vildagliptin washout. Vildagliptin administrated at doses of 10 mg/kg for 32 weeks protects
nerve fiber loss in streptozotocin (STZ)-induced diabetic adult male
Sprague Dawley rats.

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Product Categories : Proteases > DPP-4 Inhibitor