半岛bd体育手机客户端 说明
一般描述
A cell-permeable, orally bioavailable, non-toxic thiazolyl-quinolinone derived compound that acts as a potent, selective and reversible inhibitor of CD38 (IC50= 7.3 & 1.9 nM for human & mouse CD38, respectively;Ki= 0.3 nM for human wt-CD38). Shown to bind to the catalytic active site. Displays attractive PK properties in mice (p.o. 30 mg/kg: t1/2= 3.5 h, Cmax= 10.8 ?g/ml; i.v. 2 mg/kg: t1/2= 5.3 h, Cmax= 2.98 ?g/ml, Cl = 21 ml/min/kg, Vdss = 1.3 L/kg). Rapidly elevates NAD levels by several folds in both liver and gastrocnemius tissue in a diet induced obese mouse (30 mg/kg, p.o.).
生化/生理作用
Cell permeable: yes
Primary Target
CD38
Target IC50: 7.3 & 1.9 nM for human & mouse CD38, respectively
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
其他说明
Haffner, C.D., et al. 2015.J. Med. Chem.58,3548.
Tarrago, M.G., et al. 2018Cell. Metab.27,1081.
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 | C22H27N3O3S |
| 分子量 | 413.53 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze protect from light |
| 颜色 | light brown to brown white to light brown |
| 溶解性 | DMSO: 100 mg/mL |
| 储存温度 | 2-8℃ |
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 |
Sigma-Aldrich
m.cnreagent.com
