Azaindole 1 (BAY-549)

Catalog No.S6636 Batch:S663601

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Technical Data

Formula

C18H13ClF2N6O
Molecular Weight 402.79 CAS No. 867017-68-3
Solubility (25°C)* In vitro DMSO 81 mg/mL (201.09 mM)
Ethanol 2 mg/mL (4.96 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.05mg/ml Taking the 1 mL working solution as an example, add 50 μL of 81 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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)

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.