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 µg/ml; i.v. 2 mg/kg: t1/2 = 5.3 h, Cmax = 2.98 µg/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.).
Synonyms: CD38 Inhibitor - CAS 1700637-55-3 - Calbiochem; Compound 78c, CD38i_78c, 78c, Cluster of Differentiation 38 Inhibitor
Molecular Formula: C22H27N3O3S
Molecular Weight: 413.53
Linear Structural Formula: C22H27N3O3S
Purity: >=98% (HPLC)
Biochem Physiol Actions: Target IC50: 7.3 & 1.9 nM for human & mouse CD38, respectively
Legal Information: CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes: Haffner, C.D., et al. 2015. J. Med. Chem.58, 3548.Tarrago, M.G., et al. 2018 Cell. Metab.27, 1081.