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CD38 inhibitor 3 (compound 1) is the orally active inhibitor for CD38 (IC50=11 nM), that increases intracellular NAD+ levels, activates the Nrf2 signaling pathway, and promotes mitochondrial biogenesis, thereby improving muscle function[1]. | [in vivo]
CD38 inhibitor 3 (0.1-1 mg/kg, po, once daily for 58 days) inhibits NAD+ levels in muscle tissues, reduces the lactate accumulation in muscles of mice after exercise, improves the exercise endurance of Pus1-/- mice in a treadmill test[1].
CD38 inhibitor 3 exhibits good pharmacokinetics characteristics in mice, with an oral bioavailability of 61% and an AUC of 167,761 h·ng/mL[1]. | Animal Model: | Pus1-/- mouse models[1] | | Dosage: | 0.1-1 mg/kg | | Administration: | po, once daily for 58 days | | Result: | Improved the exercise endurance in a treadmill test. |
| [References]
[1] Li Y, et al. Discovery of a First-in-Class CD38 Inhibitor for the Treatment of Mitochondrial Myopathy. J Med Chem. 2023 Sep 11.. . DOI:10.1021/acs.jmedchem.3c00391 |
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