(R)-4-(1-Aminoethyl)-N-1H-pyrrolo[2,3-b]pyridin-4-ylbenzamide
(R)-4-(1-Aminoethyl)-N-1H-pyrrolo[2,3-b]pyridin-4-ylbenzamide Basic information
- Product Name:
- (R)-4-(1-Aminoethyl)-N-1H-pyrrolo[2,3-b]pyridin-4-ylbenzamide
- Synonyms:
-
- (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:
- 199433-58-4
- MF:
- C16H16N4O
- MW:
- 280.32
- Mol File:
- 199433-58-4.mol
(R)-4-(1-Aminoethyl)-N-1H-pyrrolo[2,3-b]pyridin-4-ylbenzamide Chemical Properties
- Boiling point:
- 588.8±50.0 °C(Predicted)
- Density
- 1.32
- storage temp.
- Store at -20°C
- solubility
- DMSO : 50 mg/mL (178.37 mM; Need ultrasonic and warming)H2O : < 0.1 mg/mL (insoluble)
- form
- Powder
- pka
- 11.13±0.20(Predicted)
(R)-4-(1-Aminoethyl)-N-1H-pyrrolo[2,3-b]pyridin-4-ylbenzamide Usage And Synthesis
Definition
ChEBI: 4-[(1R)-1-aminoethyl]-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide is a pyrrolopyridine.
Biological Activity
Y-33075 is a potent ROCK inhibitor derived from Y-27632, but more active with IC50 value of 3.6 nM.
in vitro
Y-33075 (Y-39983) is a potent ROCK inhibitor, with an IC 50 of 3.6 nM. It 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 are 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. It (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.
p>
target
| ROCK 3.6 nM (IC 50 ) | PKC 420 nM (IC 50 ) | CaMKII 810 nM (IC 50 ) |
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