CMPD101
| 中文名称 | CMPD101 |
|---|---|
| 中文同义词 | 化合物CMPD101;CMPD101,GRK2 / 3抑制剂;3-(((4-甲基-5-(吡啶-4-基)-4H-1,2,4-三唑-3-基)甲基)氨基)-N-(2-(三氟甲基)苄基)苯甲酰胺 |
| 英文名称 | CMPD101 |
| 英文同义词 | CMPD101;3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide;Benzamide, 3-[[[4-methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]-;Takeda101;Takeda compound 101;Rho-associated kinase,Rho-kinase,ROK,PKC,CMPD 101,desensitization,Inhibitor,inhibit,failure,CMPD101,Neuron,ROCK,Protein kinase C,heart,CMPD-101,Rho-associated protein kinase |
| CAS号 | 865608-11-3 |
| 分子式 | C24H21F3N6O |
| 分子量 | 466.46 |
| EINECS号 | |
| 相关类别 | 对照品 |
| Mol文件 | 865608-11-3.mol |
| 结构式 |  |
CMPD101 性质
| 熔点 | >80°C (dec.) |
|---|---|
| 储存条件 | -20°C Freezer |
| 溶解度 | 可溶于DMSO（少许）、甲醇（少许） |
| 形态 | 固体 |
| 颜色 | 灰白色至浅黄色 |
|
GRK2 18 nM (IC 50 ) |
GRK3 5.4 nM (IC 50 ) |
PKCα 8.1 μM (IC 50 ) |
ROCK2 1.4 μM (IC 50 ) |
CMPD101 (100 μM; pre-20 mins) inhibit the internalization of β2AR, remarkably decreases the isoproterenol-induced formation of clathrin-coated vesicles and the β2AR-GFP fusion protein remained on the plasma membrane in HEK-B2 cell line. CMPD101 (3-30 μM; pre-30 minutes) produced a robust phosphorylation of Ser375, which is partially inhibited by pretreatment of cells for 30 minutes with 3 μM Cmpd101 and fully blocked by pretreatment with 30 μM Cmpd101. It also inhibits phosphorylation of MOPr at Thr370, Thr376, and Thr379 residues. CMPD101 (3-30 μM; pre-30 minutes) does not affect the DAMGO-induced increase in ERK1/2 and Elk-1 phosphorylation, at 30 μM, this compound produces a small increase in basal ERK1/2 phosphorylation in HEK 293 cells expressing HA-MOPrs.
Western Blot Analysis
| Cell Line: | HEK 293 cells stably expressing HA-tagged rat MOPr |
| Concentration: | 3 μM, 30 μM |
| Incubation Time: | Pre-30 minutes |
| Result: | Surpressed Ser375 expression completely at a high dose. |
Western Blot Analysis
| Cell Line: | HEK 293 cells stably expressing HA-tagged rat MOPr |
| Concentration: | 3 μM, 30 μM |
| Incubation Time: | Pre-30 minutes |
| Result: | Had no effect on DAMGO-induced p-ERK1/2 and p-Elk-1 expression. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-103045 | CMPD101 CMPD101 | 865608-11-3 | 1mg | 609元 |
| 2024/01/25 | HY-103045 | CMPD101 | 5 mg | 1600元 |