产品说明
一般描述
A selective inhibitor of βARK1 (β-Adrenergic Receptor Kinase 1) (IC50 = 126 µM). Has no inhibitory activity against protein kinase A (PKA).
A selective inhibitor of β-adrenergic receptor kinase 1 (βARK1) (IC50 = 126 µM). Displays no inhibitory activity against protein kinase A (PKA). Identified from a group of existing compounds (not previously demonstrated to inhibit βARK1) using a two-step rational drug design protocol that included molecular modeling and comparative docking studies. Represents the first inhibitor that distinguishes between βARK1 and PKA, an enzyme with a similar adenine binding pocket. May be useful in the study of mechanisms involved in congestive heart failure where elevated levels of βARK1 desensitize agonist-bound β2-adrenergic receptors.
包装
5 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Primary Target
βARK1 (β-Adrenergic Receptor Kinase 1)
Product does not compete with ATP.
Reversible: no
Target IC50: 126 µM against βARK1 (β-Adrenergic Receptor Kinase 1)
Cell permeable: no
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
Iino, M., et al. 2002. J. Med. Chem.45, 2150.
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 | C12H9NO6 |
| 分子量 | 263.20 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥97% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze protect from light |
| 颜色 | yellow to orange |
| 溶解性 | DMSO: 5 mg/mL methanol: soluble |
| 运输 | ambient |
| 储存温度 | −20℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 1 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
