(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 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Definition

  ChEBI: 4-[(1R)-1-aminoethyl]-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide is a pyrrolopyridine.

• Biologische Aktivität

  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.

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• target

  ROCK 3.6 nM (IC 50 )

  PKC 420 nM (IC 50 )

  CaMKII 810 nM (IC 50 )

(R)-4-(1-Aminoethyl)-N-1H-pyrrolo[2,3-b]pyridin-4-ylbenzamide Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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