Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC 50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes
In Vitro
Ruboxistaurin mesylate inhibits PKC isozymes with IC 50 values of 0.36, 0.0047, 0.0059, 0.30, 0.25, 0.60 and 0.052 μM for PKCα, PKCβI, PKCβII, PKCγ, PKCδ, PKCε and PKCη, respectively. Ruboxistaurin mesylate inhibits Ca calmodulin and Rat Brain PKC with IC 50 values of 6.2 and 0.32 μM, respectively. Ruboxistaurin mesylate (10 and 400 nM; 4 days) significantly suppresses glucose-induced monocyte adherence under normoglycemic (NG) conditions. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Ruboxistaurin mesylate (0.1, 1.0 and 10.0 mg/kg; oral administration, once daily for 4 weeks) decreases the increasing of leukocyte entrapment in the retinal microcirculation during the early diabetes period. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male long-evans rats with streptozotocin induced diabetesDosage: 0.1, 1.0 and 10.0 mg/kg Administration: Oral administration; 0.1, 1.0 and 10.0 mg/kg, once daily for 4 weeks Result: Significantly decreased the number of leukocytes in the retinal microcirculation of rats with streptozotocin induced diabetes.
Form:Solid
IC50& Target:PKC-βI 4.7 nM (IC 50 ) PKC-βII 5.9 nM (IC 50 ) PKCη 52 nM (IC 50 ) PKCδ 250 nM (IC 50 ) PKCγ 300 nM (IC 50 ) PKCα 360 nM (IC 50 ) PKCε 600 nM (IC 50 )
