199433-58-4

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

英文名称 (R)-4-(1-Aminoethyl)-N-1H-pyrrolo[2,3-b]pyridin-4-ylbenzamide

CAS 199433-58-4

分子式 C16H16N4O

分子量 280.32

MOL 文件 199433-58-4.mol

199433-58-4 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

(R)-4-(1-氨基乙基)-N-1H-吡咯并[2,3-B]吡啶-4-基苯甲酰胺

英文别名

Y 33075
Y 39983
Y39983
Y33075
Y 39983
(R)-4-(1-Aminoethyl)-N-1H-pyrrolo[2,3-b]pyridin-4-ylbenzamide
4-[(1R)-1-Aminoethyl]-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide
Benzamide, 4-[(1R)-1-aminoethyl]-N-1H-pyrrolo[2,3-b]pyridin-4-yl-
(R)-4-(1-Aminoethyl)-N-1H-pyrrolo[2,3-b]pyridin-4-ylbenzamide ISO 9001：2015 REACH

所属类别

医药中间体：乙基吡啶

物理化学性质

沸点588.8±50.0 °C(Predicted)

密度1.32

储存条件-20°C储存

溶解度DMSO : 50 mg/mL (178.37 mM; Need ultrasonic and warming)H2O : < 0.1 mg/mL (insoluble)

酸度系数(pKa)11.13±0.20(Predicted)

形态粉末

常见问题列表

生物活性

Y-33075 是一种有效的 ROCK 抑制剂，源于 Y-27632，但活性更强，IC50 值 3.6 nM。

靶点

ROCK

3.6 nM (IC ₅₀ )

PKC

420 nM (IC ₅₀ )

CaMKII

810 nM (IC ₅₀ )

体外研究

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.

体内研究

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.