5.31230

Troponin Activator, CK-2017357

• 別名: Troponin Activator, CK-2017357, 6-Ethynyl-1-(3-pentanyl)-1H-imidazo[4,5-b]pyrazin-2-ol, 6-Ethynyl-1-(pentan-3-yl)-1H-imidazo[4,5-b]pyrazin-2-ol, Fast Skeletal Troponin Activator, CK2017357, Tirasemtiv, CK-357, Tirasemtiv, CK-357, 6-Ethynyl-1-(3-pentanyl)-1H-imidazo[4,5-b]pyrazin-2-ol, 6-Ethynyl-1-(pentan-3-yl)-1H-imidazo[4,5-b]pyrazin-2-ol, Fast Skeletal Troponin Activator, CK2017357
• 実験式（ヒル表記法）: C₁₂H₁₄N₄O
• CAS番号: 1005491-05-3
• 分子量: 230.27
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: powder
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: beige
• 溶解性: DMSO: 25 mg/mL
• 保管温度: 2-8°C
• InChI: 1S/C12H14N4O/c1-4-8-7-13-10-11(14-8)16(12(17)15-10)9(5-2)6-3/h1,7,9H,5-6H2,2-3H3,(H,13,15,17)
• InChI Key: RSQGZEAXODVTOL-UHFFFAOYSA-N

詳細

詳細

An orally bioavailable, non-toxic imidazopyrazinol compound that directly and selectively binds to the troponin complex in fast skeletal muscle (K_d = 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 (K_d = 3.8 µM) 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^-1 to 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.

An orally bioavailable, non-toxic imidazopyrazinol compound that directly and selectively binds to the troponin complex in fast skeletal muscle (K_d = 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 (K_d = 3.8 µM) 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^-1 to 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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
troponin complex

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C).

その他情報

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.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable