CD38 INHIBITOR 1PC X 10MG

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.).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
CD38

Reversible: yes

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Haffner, C.D., et al. 2015. J. Med. Chem.58, 3548.
Tarrago, M.G., et al. 2018 Cell. Metab.27, 1081.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany