CD38 inhibitor 78c

Biological Activity

CD38 inhibitor 78c is a potent CD38 (ADP ribosyl cyclase/hydrolase) inhibitor (IC₅₀ values are 1.9 and 7.3 nM at mouse and human CD38, respectively). Catalyzes breakdown of NAD to nicotinamide and ADPR, and hydrolyzes NAADP to adenosine-5'-O-diphosphoribose phosphate. Elevates NAD⁺ levels >5-fold in liver and >1.2-fold in muscle of diet-induced obese (DIO) C57Bl6 mice. Also prevents age-related NAD⁺ decline in mice. Improves glucose intolerance, cardiac function and improves physiological and metabolic parameters in old mice.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. A potent and specific CD38 inhibitor ameliorates age-related metabolic dysfunction by reversing tissue NAD⁺ decline.
   Tarrago et al.
   Cell Metab., 2018;27:1081
2. Discovery, synthesis, and biological evaluation of thiazoloquin(az)olin(on)es as potent CD38 inhibitors.
   Haffner et al.
   J.Med.Chem., 2015;58:3548

Product Datasheets