Inhibition of recombinant mouse wild-type NAMPT expressed in bacterial expression system using PRPP as substrate in presence of mouse NMNAT-3 measured for 1 hr by fluorescence assay
Metabolic stability in Wistar Han rat liver microsomes assessed as parent compound remaining at 50 uM in absence of NADPH for 60 mins by LC-ESI/MS analysis
Toxicity in Crl:CD Sprague-Dawley rat retina at 100 mg/kg, ip administered once daily for 5 days by hematoxylin and eosin staining based microscopic analysis
Toxicity in Crl:CD Sprague-Dawley rat heart assessed as hypereosinophilia at 100 mg/kg, ip administered once daily for 5 days by hematoxylin and eosin staining based microscopic analysis
Toxicity in Crl:CD Sprague-Dawley rat heart assessed as increase in cardiomyocytes cytoplasmic vacuolation at 100 mg/kg, ip administered once daily for 5 days by hematoxylin and eosin staining based microscopic analysis
Toxicity in Crl:CD Sprague-Dawley rat heart assessed as interstitial expansion at 100 mg/kg, ip administered once daily for 5 days by hematoxylin and eosin staining based microscopic analysis
Antitumor activity against mouse 4T1 cells implanted in BALB/c mouse assessed as reduction in tumour volume at 10 mg/kg, ip bid for 12 days by vernier caliper method
Antitumor activity against mouse 4T1 cells implanted in Balb/c mouse mouse assessed as inhibition of tumor metastasis at 10 mg/kg, ip bid for 12 days measured post last dose by crystal violet staining based thioguanine clonogenic assay