For research use only. Not for therapeutic Use.
MK-0159 is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD+ (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart[1].
MK-0159 (compound 37) (0-50 μM, 24 h) increases both extracellular and intracellular NAD+ in A549 cells and HMVEC cells[1].
MK-0159 (20 μM, overnight) reduces the number of cells with damaged mitochondria in CD38-overexpressing CD8+ T cells[2].
MK-0159 (3-30 mg/kg, p.o., a single dose) increases systemic NAD+ and decreases ADPR levels (the product and substrate of CD38 enzymatic activity) in blood and heart of mice[1].
MK-0159 (30 mg/kg, p.o.) reduces infarct size in cardiac I/R injury mice[2].
MK-0159 (30 mg/kg, oral gavage, twice a day for 9 days) reverses mitochondrial defect, restores CD8+ T cell function and inhibits virally induced organ inflammation in BXD2 lupus-prone mice with LCMV infection[2].
| Catalog Number | I043337 |
| CAS Number | 2641484-61-7 |
| Synonyms | N-[4-(2-methoxyethoxy)cyclohexyl]-6-(1,3-thiazol-5-yl)-1H-pyrrolo[2,3-b]pyridine-4-carboxamide |
| Molecular Formula | C20H24N4O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C20H24N4O3S/c1-26-8-9-27-14-4-2-13(3-5-14)23-20(25)16-10-17(18-11-21-12-28-18)24-19-15(16)6-7-22-19/h6-7,10-14H,2-5,8-9H2,1H3,(H,22,24)(H,23,25) |
| InChIKey | JUVJFMVGYBBDKN-UHFFFAOYSA-N |
| SMILES | COCCOC1CCC(CC1)NC(=O)C2=CC(=NC3=C2C=CN3)C4=CN=CS4 |
| Reference | [1]. Lagu B, et al. Orally Bioavailable Enzymatic Inhibitor of CD38, MK-0159, Protects against Ischemia/Reperfusion Injury in the Murine Heart. J Med Chem. 2022 Jun 28. [2]. Chen PM, et al. CD38 reduces mitochondrial fitness and cytotoxic T cell response against viral infection in lupus patients by suppressing mitophagy. Sci Adv. 2022 Jun 17;8(24):eabo4271. |
