| Identification | Back Directory | [Name]
3(2H)-Pyridazinone, 2-[(5-fluoro-3-pyridinyl)methyl]-6-[2-(2,2,2-trifluoroethoxy)-5-pyrimidinyl]- | [CAS]
2417395-15-2 | [Synonyms]
Sevasemten
2-[(5-fluoro-3-pyridinyl)methyl]-6-[2-(2,2,2-trifluoroethoxy)-5-pyrimidinyl]-3(2H)-Pyridazinone
3(2H)-Pyridazinone, 2-[(5-fluoro-3-pyridinyl)methyl]-6-[2-(2,2,2-trifluoroethoxy)-5-pyrimidinyl]- | [Molecular Formula]
C16H11F4N5O2 | [MOL File]
2417395-15-2.mol | [Molecular Weight]
381.28 |
| Chemical Properties | Back Directory | [Boiling point ]
498.1±55.0 °C(Predicted) | [density ]
1.49±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
2.32±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Sevasemten is an orally active allosteric inhibitor of skeletal muscle myosin that protects skeletal muscle from contraction-induced injury. Sevasemten exhibits selectively myosin inhibition with IC50s of ≤10 μM (skeletal), >100 μM (cardiac), respectively. Sevasemten decreases muscle damage biomarkers and fibrosis while increasing muscle strength and activity in in Duchenne muscular dystrophy disease models[1][2][3][4]. | [References]
[1] Russell Alan, et al. Preparation of substituted pyridazinones for use in the treatment of neuromuscular diseases: World Intellectual Property Organization, WO2021231615. 2021-11-18.
[2] WHO Drug Information-World Health Organization (WHO).
[3] Donovan J, et al. 351P Sevasemten, a fast myosin inhibitor, in adults with Becker muscular dystrophy results in reduced muscle damage biomarkers and functional stabilization[J]. Neuromuscular Disorders, 2024, 43: 104441.682.
[4] Russell AJ, et al., Modulating fast skeletal muscle contraction protects skeletal muscle in animal models of Duchenne muscular dystrophy. J Clin Invest. 2023 May 15;133(10):e153837. |
|
|