(R)-4-(1-氨基乙基)-N-1H-吡咯并[2,3-B]吡啶-4-基苯甲酰胺
| 中文名称 | (R)-4-(1-氨基乙基)-N-1H-吡咯并[2,3-B]吡啶-4-基苯甲酰胺 |
|---|---|
| 中文同义词 | (R)-4-(1-氨基乙基)-N-1H-吡咯并[2,3-B]吡啶-4-基苯甲酰胺;化合物 T13384 |
| 英文名称 | (R)-4-(1-Aminoethyl)-N-1H-pyrrolo[2,3-b]pyridin-4-ylbenzamide |
| 英文同义词 | (R)-4-(1-Aminoethyl)-N-1H-pyrrolo[2,3-b]pyridin-4-ylbenzamide;Y 33075;Y33075;Y 39983;Y 39983;Y39983;Benzamide, 4-[(1R)-1-aminoethyl]-N-1H-pyrrolo[2,3-b]pyridin-4-yl-;4-[(1R)-1-Aminoethyl]-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide;(R)-4-(1-Aminoethyl)-N-1H-pyrrolo[2,3-b]pyridin-4-ylbenzamide ISO 9001：2015 REACH;Y 33075,Y33075 |
| CAS号 | 199433-58-4 |
| 分子式 | C16H16N4O |
| 分子量 | 280.32 |
| EINECS号 | |
| 相关类别 | 细胞周期 |
| Mol文件 | 199433-58-4.mol |
| 结构式 | ![(R)-4-(1-氨基乙基)-N-1H-吡咯并[2,3-B]吡啶-4-基苯甲酰胺 结构式](CAS2/GIF/199433-58-4.gif) |
(R)-4-(1-氨基乙基)-N-1H-吡咯并[2,3-B]吡啶-4-基苯甲酰胺 性质
| 沸点 | 588.8±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.32 |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO：50 mg/mL（178.37 mM；需要超声波和加热）H2O：< 0.1 mg/mL（不溶） |
| 形态 | 粉末 |
| 酸度系数(pKa) | 11.13±0.20(Predicted) |
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ROCK 3.6 nM (IC 50 ) |
PKC 420 nM (IC 50 ) |
CaMKII 810 nM (IC 50 ) |
Y-33075 (Y-39983) is a potent ROCK inhibitor, with an IC 50 of 3.6 nM. Y-33075 also inhibits PKC and CaMKII more potently than Y-27632, and the IC 50 s of Y-27632 and Y-33075 for PKC are 9.0 μM and 0.42 μM, respectively, whereas the IC 50 s of Y-27632 and Y-33075 for CaMKII are 26 μM and 0.81 μM, respectively. The IC 50 s of Y-27632 and Y-33075 for PKC is 82 and 117 times those for ROCK, respectively, whereas the IC 50 s of Y-27632 and Y-33075 for CaMKII is 236 and 225 times those for ROCK, respectively. Y-33075 (Y-39983, 10 μM) extends neurites in the retinal ganglion cells (RGCs) compared with those in RGCs treated without Y-39983. Y-33075 (Y-39983, 1 μM) inhibits the contraction of rabbit ciliary artery segments evoked by histamine in Ca 2+ -free solutions. Y-33075 (10 μM) shows no effect on the [Ca 2+ ]i increase with the high-potassium (high-K) solution.
In rabbits, Y-39983 (≥0.01%) significantly lowers intraocular pressure (IOP) at 2 hours after topical administration. In monkeys, Y-39983 (0.05%)-treated eyes show significant reduction of IOP between 2 and 7 hours after topical administration. Y-39983 (100 μM) increases the regenerating axons of retinal ganglion cells (RGCs) in the eyes of the rats.