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首页-小分子抑制剂&激动剂-Cytoskeleton/Cell Adhesion Molecules-Myosin-EDG-5506
EDG-5506

Chemical Structure : EDG-5506

CAS No.: 2417395-15-2

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EDG-5506 (Sevasemten, EDG5506, EDG 5506)

货号: PC-20390Not For Human Use, Lab Use Only.

EDG-5506 (Sevasemten) is a potent, selective, orally active inhibitor of fast skeletal muscle myosin, inhibits fast myofibril ATPase from rabbit psoas muscle with IC50 of 0.2 uM.

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10 mg ￥1880 In stock
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50 mg ￥5280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

EDG-5506 (Sevasemten) is a potent, selective, orally active inhibitor of fast skeletal muscle myosin, inhibits fast myofibril ATPase from rabbit psoas muscle with IC50 of 0.2 uM.
EDG-5506 is inactive against cardiac and slow bovine masseter skeletal myofibrils with an IC50 greater than 100 uM.
EDG-5506 is also a potent inhibitor of other mixed fast myosin myofibrils (mouse gastroc IC50 0.4 uM, 21% IIa, 15% IIx, 56%IIb; mouse TA IC50 0.4 uM, mixed IIa, IIx, IIb suggesting equal potency against all fast skeletal myosin proteins.
EDG-5506 inhibits the enzymatic activity of fast skeletal S1 from rabbit psoas but not porcine ventricular cardiac S1 or the more unrelated smooth muscle S1 with an IC50 of 0.11 uM and >100 uM, respectively.
EDG-5506 effectively reduces dye uptake in ex vivo lengthening contraction of mdx EDL muscle using a membrane-impermeable dye.
EDG-5506 protects skeletal muscle in mdx and DBA/2 mdx mice in vivo, with no effect on body or muscle weight.
EDG-5506 lowers disease biomarkers and improves physical function in duchenne muscular dystrophy (DMD) dogs.

物理化学性质&存储条件

分子量 381.29
分子式 C16H11F4N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-((5-fluoropyridin-3-yl)methyl)-6-(2-(2,2,2-trifluoroethoxy)pyrimidin-5-yl)pyridazin-3(2H)-one

参考文献

1. Russell AJ, et al. J Clin Invest. 2023 Mar 30:e153837.

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