Azaindole 1 (TC-S 7001)

Catalog No.S6636

For research use only.

Azaindole 1 (TC-S 7001) 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 (TC-S 7001) Chemical Structure

CAS No. 867017-68-3

Purity & Quality Control

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Biological Activity

Description Azaindole 1 (TC-S 7001) 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

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

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]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 402.79
Formula

C18H13ClF2N6O

CAS No. 867017-68-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CNC2=NC=CC(=C12)OC3=C(C=C(C=C3F)NC4=CC(=NC(=N4)N)Cl)F

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

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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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