Sigma Aldrich Fine Chemicals Biosciences CD38 Inhibitor - CAS 17006

Supplier:  Sigma Aldrich Fine Chemicals Biosciences 5387630001

A cell-permeable orally bioavailable non-toxic thiazolyl-quinolinone derived compound that acts as a potent selective and reversible inhibitor of CD38 (IC50 7.3 1.9 nM for human mouse CD38 respectively Ki 0.3 nM for human wt-CD38). Shown to bind to the catalytic active site. Displays attractive PK properties in mice (p.o. 30 mg/kg t1/2 3.5 h Cmax 10.8 181g/ml i.v. 2 mg/kg t1/2 5.3 h Cmax 2.98 181g/ml Cl 21 ml/min/kg Vdss 1.3 L/kg). Rapidly elevates NAD levels by several folds in both liver and gastrocnemius tissue in a diet induced obese mouse (30 mg/kg p.o.).

Catalog No. 50-289-7325