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; 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.).
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)
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