半岛bd体育手机客户端 说明
一般描述
An orally bioavailable, non-toxic imidazopyrazinol compound that directly and selectively binds to the troponin complex in fast skeletal muscle (Kd= 40 nM) and sensitizes it to calcium. Its binding site is believed to be between two or more troponin subunits. Exhibits very modest affinity for slow skeletal muscle troponin (Kd= 3.8 ?M) and has no measurable affinity for cardiac muscle troponin. Effectively stimulates myosin ATPase activity in fast skeletal muscle (EC50= 390 nM), but has significantly reduced effect on mixed fiber type (EC50= 770 nM in bovine rectus abdominis muscle). Slows the first order rate constant for Ca2+release by about 70% (from 14.7 s-1to 4.0 s-1) and shifts the plot of myosin ATPase relationship to calcium leftwards in fast skeletal muscles without increasing the maximum recorded force or the shape of the curve. Shown to improve muscle function in a rodent model of neuromuscular disease where neural input is diminished.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
An orally bioavailable, non-toxic imidazopyrazinol compound that directly and selectively binds to the troponin complex in fast skeletal muscle (Kd= 40 nM) and sensitizes it to calcium. Its binding site is believed to be between two or more troponin subunits. Exhibits very modest affinity for slow skeletal muscle troponin (Kd= 3.8 ?M) and has no measurable affinity for cardiac muscle troponin. Effectively stimulates myosin ATPase activity in fast skeletal muscle (EC50= 390 nM), but has significantly reduced effect on mixed fiber type (EC50= 770 nM in bovine rectus abdominis muscle). Slows the first order rate constant for Ca2+release by about 70% (from 14.7 s-1to 4.0 s-1) and shifts the plot of myosin ATPase relationship to calcium leftwards in fast skeletal muscles without increasing the maximum recorded force or the shape of the curve. Shown to improve muscle function in a rodent model of neuromuscular disease where neural input is diminished.
生化/生理作用
Cell permeable: yes
Primary Target
troponin complex
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C).
其他说明
Gordon, P., et al. 2013.Expert Opin. Phamacother.14,1907.
Miciak, J.J., et al. 2013.Muscle Nerve.48,279.
Russell, A.J., et al. 2012.Nat. Med.18,452.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C12H14N4O |
分子量 | 230.27 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | powder |
manufacturer/tradename | Calbiochem? |
储存条件 | OK to freeze protect from light |
颜色 | beige |
溶解性 | DMSO: 25 mg/mL |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich