5.05479

SIRT1/2/3 pan Inhibitor

• 别名: SIRT1/2/3 pan Inhibitor, 4-(4-(2-Pivalamidoethyl)piperidin-1-yl)thieno[3,2-d]pyrimidine-6-carboxamide, pan SIRT1/2/3 Inhibitor, pan SIRT1/2/3 Inhibitor, 4-(4-(2-Pivalamidoethyl)piperidin-1-yl)thieno[3,2-d]pyrimidine-6-carboxamide
• 经验公式（希尔记法）: C₁₉H₂₇N₅O₂S
• CAS号: 1431411-60-7
• 分子量: 389.51
• MDL编号: MFCD00149973
• UNSPSC代码: 12352200
• NACRES: NA.77

属性

• 方案: ≥97% (HPLC)
• 质量水平: 100
• 表单: powder
• 制造商/商品名称: Calbiochem^®
• 储存条件: OK to freeze; protect from light
• 颜色: pale yellow
• 溶解性: DMSO: 10 mg/mL
• 储存温度: 2-8°C

说明

一般描述

A thienopyrimidinylcarboxamide that acts as a highly potent, reversible pan sirtuin (SIRT) inhibitor (IC₅₀ = 15, 10, and 33 nM for SIRT1, 2, and 3, respectively). Shown to bind to the SIRT catalytic site and occupy both the nicotinamide C-pocket and acetyl lysine substrate channel. Exhibits high selectivity over a panel of protein kinases, nuclelar receptors, GPCRs, and ion-channels (IC₅₀ >10 µM). Poorly affects hERG and cytochrome P450s (>50 µM). Exhibits desirable stability in microsomal preparations (human CL_int = 15.8 µL/min/mg, mouse CL_int = 12.7 µL/min/mg) and high solubility (297 µM), and low LogD (2.73).

生化/生理作用

Primary Target
SIRT1/2/3

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

Disch, J.S., et al. 2013. J. Med. Chem.57, 1275.

法律信息

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

安全信息

• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 2
• 闪点(°F): Not applicable
• 闪点(°C): Not applicable