5.31230

Troponin Activator, CK-2017357

• 别名: 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
• 经验公式（希尔记法）: C₁₂H₁₄N₄O
• CAS号: 1005491-05-3
• 分子量: 230.27
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• 化驗: ≥98% (HPLC)
• 品質等級: 100
• 形狀: powder
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: beige
• 溶解度: DMSO: 25 mg/mL
• 儲存溫度: 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 密鑰: RSQGZEAXODVTOL-UHFFFAOYSA-N

说明

一般說明

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.

生化／生理作用

Cell permeable: yes

Primary Target
troponin complex

Reversible: yes

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

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

其他說明

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.

法律資訊

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

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable