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| | CD38 inhibitor 3 Basic information |
| Product Name: | CD38 inhibitor 3 | | Synonyms: | CD38 inhibitor 3;4-Pyrimidinecarboxamide, 2-(1H-imidazol-1-yl)-N-[2-(2-methoxyethoxy)-5-pyrimidinyl]-6-(trifluoromethyl)-;IPG8294 | | CAS: | 2857868-82-5 | | MF: | C16H14F3N7O3 | | MW: | 409.32 | | EINECS: | | | Product Categories: | | | Mol File: | 2857868-82-5.mol |  |
| | CD38 inhibitor 3 Chemical Properties |
| density | 1.533±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | pka | 8.353±0.70(predicted) | | form | Solid | | color | White to light yellow |
| | CD38 inhibitor 3 Usage And Synthesis |
| Uses | 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 |
| | CD38 inhibitor 3 Preparation Products And Raw materials |
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