5.34377

CMB-087229

• 别名: CMB-087229, 5-[(3,5-Dichlorophenoxy)methyl]-1,2-dihydro-3H-pyrazol-3-one, CMB087229
• 经验公式（希尔记法）: C₁₀H₈Cl₂N₂O₂
• CAS号: 1227692-67-2
• 分子量: 259.09
• MDL编号: MFCD31745789
• UNSPSC代码: 12352200
• PubChem化学物质编号: 45102767
• NACRES: NA.77

属性

• 方案: ≥98% (HPLC)
• 质量水平: 100
• 表单: solid
• 制造商/商品名称: Calbiochem^®
• 储存条件: OK to freeze; protect from light
• 颜色: white
• 溶解性: DMSO: 50 mg/mL
• 储存温度: 2-8°C
• SMILES字符串: C1=C(C=C(C=C1Cl)Cl)OCC2=CC(=O)NN2

说明

一般描述

A cell-permeable, blood-brain barrier permeable, non-toxic pyrazolone compound that potently blocks mutant Cu/Zn SOD1 cytotoxicity (EC₅₀ = 67 nM in PC12 cells expressing mutant G93A SOD1). Shown to directly interact with 26S proteasome PSMC1 and PSMC4 and the chaperone protein TCP-1 and enhance proteasome activity. Offers neuroprotection against protein aggregation induced toxicity and prolongs the survival of ALS transgenic mice by 13.3% (20 mg/kg, i.p., q.d.) Demonstrates attractive microsomal (T_1/2 = 93 & 36 min in human & mouse, respectively) and metabolic stability, aqueous solubility (250 µM) and PK profile in mice. Poorly affects the activities of 68-enzymes & receptors, hERG and Cyp450 isozymes at 10 µM.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

生化/生理作用

Cell permeable: yes

Primary Target
26S proteasome PSMC1 and PSMC4 and the chaperone protein TCP-1

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 3 months at -20°C.

其他说明

Tripper, P.C., et al. 2014. ACS Chem. Neurosci.5, 823.
Chen, T., et al. 2012. J. Med. Chem.55, 515.

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 3
• 闪点(°F): Not applicable
• 闪点(°C): Not applicable