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MPH-220

Names

[ CAS No. ]:
2649776-79-2

[ Name ]:
MPH-220

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Cytoskeleton >> Myosin
Research Areas >> Neurological Disease

[In Vitro]

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]。

[In Vivo]

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.

[References]

[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.  

Chemical & Physical Properties

[ Molecular Formula ]:
C20H21N3O3S

[ Molecular Weight ]:
383.46

Related Compounds