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ROCK-IN-2

Name: ROCK-IN-2
Brand: TargetMol
SKU: TQ0110
Price: 116 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0110Cas No. 867017-68-3

Alias TC-S 7001, Azaindole 1

ROCK-IN-2 (Azaindole 1) is a selective and ATP-competitive ROCK inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2.

ROCK-IN-2

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Purity: 97.29%

Catalog No. TQ0110Alias TC-S 7001, Azaindole 1Cas No. 867017-68-3

ROCK-IN-2 (Azaindole 1) is a selective and ATP-competitive ROCK inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$116	In Stock	In Stock
5 mg	$289	In Stock	In Stock
10 mg	$463	In Stock	In Stock
25 mg	$745	In Stock	In Stock
50 mg	$1,060	In Stock	In Stock
100 mg	$1,430	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$389	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:97.29%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	ROCK-IN-2 (Azaindole 1) is a selective and ATP-competitive ROCK inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2.
Targets&IC50	ROCK2:1.1 nM (cell free), ROCK1:0.6 nM (cell free)
In vitro	Azaindole 1 a highly potent inhibitor of human ROCK-1 and ROCK-2 (IC50s: 0.6 and 1.1?nM) and also inhibits murine ROCK-2 or rat ROCK-2 (IC50s: 2.4 and 0.8?nM). Azaindole 1 also inhibits receptor tyrosine kinases TRK and FLT3, with IC50s of 252 and 303?nM, respectively, but shows slight inhibition of MLCK and ZIP-kinase with IC50s of 7.4?μM and 4.1?μM, respectively. Azaindole 1 induces vasorelaxation in vitro and suppresses the phenylephrine-induced contraction of the rabbit saphenous artery in a concentration-dependent manner (IC50: 65?nM).
In vivo	Azaindole 1 (0.03, 0.1, 0.3?mg/kg, i.v.) results in a dose-dependent and long-lasting decrease in blood pressure in anaesthetized normotensive rats. Azaindole 1 (3 and 10?mg/kg, p.o.) decreases blood pressure dose-dependently and persistently both in normotensive and hypertensive rats and shows such effects even at 1?mg/kg in hypertensive rats. Azaindole 1 (0.1 and 0.3?mg/kg, i.v. bolus injections) causes decreased mean arterial blood pressure in a dose-related manner and only leads to a moderate and dose-independent increase in heart rate of anesthetized dogs.
Animal Research	Male Wistar rats (300-350?g) are anesthetized with thiopental 100?mg/kg intraperitoneally (i.p.). A tracheotomy is performed and catheters are inserted into the femoral artery for blood pressure and heart rate measurements and into the femoral vein for test drug administration. The animals are ventilated with room air and their body temperature is controlled. Azaindole 1 is administered intravenously (i.v.) in doses of 0.03-0.1?mg/kg. The vehicle Transcutol/Cremophor EL/physiological saline (19/10/80 = v/v/v) without test drug is used as control. The volume administered is 1?mL/kg. Six animals are treated per group.
Synonyms	TC-S 7001, Azaindole 1

Chemical Properties

Molecular Weight	402.79
Formula	C₁₈H₁₃ClF₂N₆O
Cas No.	867017-68-3
Smiles	Cc1c[nH]c2nccc(Oc3c(F)cc(Nc4cc(Cl)nc(N)n4)cc3F)c12
Relative Density.	1.61

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: Insoluble

DMSO: 30 mg/mL (74.48 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (4.97 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4827 mL	12.4134 mL	24.8268 mL	124.1342 mL
5 mM	0.4965 mL	2.4827 mL	4.9654 mL	24.8268 mL
10 mM	0.2483 mL	1.2413 mL	2.4827 mL	12.4134 mL
20 mM	0.1241 mL	0.6207 mL	1.2413 mL	6.2067 mL
50 mM	0.0497 mL	0.2483 mL	0.4965 mL	2.4827 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc