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199433-58-4

中文名稱 (R)-4-(1-氨基乙基)-N-1H-吡咯并[2,3-B]吡啶-4-基苯甲酰胺
英文名稱 (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
更新日期 2024/12/03 15:40:34
199433-58-4 結(jié)構(gòu)式 199433-58-4 結(jié)構(gòu)式

基本信息

中文別名
(R)-4-(1-氨基乙基)-N-1H-吡咯并[2,3-B]吡啶-4-基苯甲酰胺
英文別名
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
所屬類別
醫(yī)藥中間體:乙基吡啶

物理化學(xué)性質(zhì)

沸點588.8±50.0 °C(Predicted)
密度1.32
儲存條件-20°C儲存
溶解度DMSO : 50 mg/mL (178.37 mM; Need ultrasonic and warming)H2O : < 0.1 mg/mL (insoluble)
酸度系數(shù)(pKa)11.13±0.20(Predicted)
形態(tài)粉末
顏色White to off-white

常見問題列表

生物活性
Y-33075 是一種有效的 ROCK 抑制劑,源于 Y-27632,但活性更強,IC50 值 3.6 nM。
靶點

ROCK

3.6 nM (IC 50 )

PKC

420 nM (IC 50 )

CaMKII

810 nM (IC 50 )

體外研究

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.

體內(nèi)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.

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