MPH-220 is a selective and orally active inhibitor of skeletal muscle myosin-2. MPH-220 enables muscle relaxation. MPH-220 is anti-spastic agent that can be used in the research of spasticity and muscle stiffness[1].
MPH-220 (0-50 µM) 抑制人肌肉肌球蛋白样品中肌动蛋白激活的 ATP 酶活性[1]。
MPH-220 (25-30 mg/kg，腹腔注射或口服灌胃) 可降低麻醉大鼠的骨骼肌力量，而不会影响心血管[1]。
MPH-220 (15 mg/kg，口服) 改善脑损伤大鼠的步态功能[1]。
| Animal Model: | Anesthetized rats[1] |
| Dosage: | 25-30 mg/kg |
| Administration: | Intraperitoneal injection (i.p.) or oral gavage |
| Result: | Reduced skeletal muscle force. Observed MPH-220 distribution in rat tissues in a time-dependent manner and a dose-dependent, few-fold accumulation in skeletal muscle. |
[1]. Gyimesi M, et al. Single Residue Variation in Skeletal Muscle Myosin Enables Direct and Selective Drug Targeting for Spasticity and Muscle Stiffness. Cell. 2020 Oct 15;183(2):335-346.e13.