865608-11-3
865608-11-3 結(jié)構(gòu)式
基本信息
Takeda101
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]-
常見問題列表
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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. |