Home Cell Cycle ROCK inhibitor Azaindole 1 (BAY-549) For research use only.

Azaindole 1 (BAY-549)

Synonyms: TC-S 7001

Azaindole 1 (BAY-549) is a selective Rho-associated protein kinase (ROCK) inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2 in an ATP-competitive manner.

Azaindole 1 (BAY-549) Chemical Structure

Azaindole 1 (BAY-549) Chemical Structure

CAS: 867017-68-3

Purity & Quality Control

Batch: S663601 DMSO] 81 mg/mL] false] Ethanol] 2 mg/mL] false] Water] Insoluble] false Purity: 98.59%
98.59

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Biological Activity

Description Azaindole 1 (BAY-549) is a selective Rho-associated protein kinase (ROCK) inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2 in an ATP-competitive manner.
Targets
ROCK1 [1]
(Cell-free assay)		 ROCK2 [1]
(Cell-free assay)
0.6 nM 1.1 nM
In vitro
In vitro

Azaindole 1 induces vasorelaxation in vitro.Azaindole 1 inhibits concentration dependently the phenylephrine-induced contraction of rabbit saphenous artery with an IC50 value of 65 nm. [1]
In Vivo
In vivo

Azaindole 1 induced a dose-dependent and long-lasting decrease in blood pressure in anaesthetized normotensive rats. i.v. administration of 0.03, 0.1, 0.3 mg kg−1, resulted in a reduction in the maximal blood pressure of 8, 18, 35 mm Hg, respectively. In normotensive rats, azaindole 1 also induced a dose-dependent and persistent decrease in blood pressure.In conscious spontaneously hypertensive rats, azaindole 1 induced a dose-dependent and long-lasting decrease in mean blood pressure after oral application.At all doses tested, azaindole 1 causes only a moderate and dose-independent increase in heart rate.[1]

Chemical lnformation & Solubility

Molecular Weight 402.79 Formula

C18H13ClF2N6O
CAS No. 867017-68-3 SDF --
Smiles CC1=CNC2=NC=CC(=C12)OC3=C(C=C(C=C3F)NC4=CC(=NC(=N4)N)Cl)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 81 mg/mL ( (201.09 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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