Biochem/physiol Actions

Reversible: yes

Target IC₅₀: 7.3 & 1.9 nM for human & mouse CD38, respectively

Primary TargetCD38

Cell permeable: yes

General description

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; K_i = 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: t_1/2 = 3.5 h, C_max = 10.8 µg/ml; i.v. 2 mg/kg: t_1/2 = 5.3 h, C_max = 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.).

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.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Warning

Toxicity: Standard Handling (A)