1. Cell Cycle/DNA Damage
    TGF-beta/Smad
    Stem Cell/Wnt
  2. ROCK
  3. Azaindole 1

Azaindole 1 (Synonyms: TC-S 7001)

Cat. No.: HY-10319 Purity: 99.46%
Handling Instructions

Azaindole 1 is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively.

For research use only. We do not sell to patients.

Azaindole 1 Chemical Structure

Azaindole 1 Chemical Structure

CAS No. : 867017-68-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 474 In-stock
Estimated Time of Arrival: December 31
5 mg USD 431 In-stock
Estimated Time of Arrival: December 31
10 mg USD 617 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1682 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2468 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Azaindole 1 is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively.

IC50 & Target[1]

ROCK-1

0.6 nM (IC50)

ROCK-2

1.1 nM (IC50)

TRK

252 nM (IC50)

FLT3

303 nM (IC50)

In Vitro

Azaindole 1 is a highly potent inhibitor of human ROCK-1 and ROCK-2, with IC50s of 0.6 and 1.1 nM, respectively, and also inhibits murine ROCK-2 or rat ROCK-2 with IC50s of 2.4 and 0.8 nM, respectively. 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 rabbit saphenous artery in a concentration dependent manner with an IC50 value of 65 nM[1].

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 anaesthetized dogs[1].

Molecular Weight

402.79

Formula

C₁₈H₁₃ClF₂N₆O

CAS No.

867017-68-3

SMILES

NC1=NC(Cl)=CC(NC2=CC(F)=C(OC3=C4C(NC=C4C)=NC=C3)C(F)=C2)=N1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (82.75 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4827 mL 12.4134 mL 24.8268 mL
5 mM 0.4965 mL 2.4827 mL 4.9654 mL
10 mM 0.2483 mL 1.2413 mL 2.4827 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

Human ROCK-1 and ROCK-2, murine ROCK-2, human ZIP-kinase and human MLC kinase (MLCK) (aa1425-1771) are preincubated for 10 min with test compounds in 0.05 mL of 50 mM Tris/HCl, pH 7.5, 1 mM EDTA, 5 mM MgCl2 and 0.06% CHAPS or 50 mM HEPES, pH 7.4, 10 mM Mg acetate, 1 mM dithiothreitol, 0.3 mM CaCl2, 1 μM calmodulin (MLCK). As substrate following peptides are used: RRLSSLRA (ROCK; S6 peptide), KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK (ZIP-kinase; long S6 peptide) and KKRAARATSNVFA (MLCK; MLC peptide). After 10 min preincubation with dimethyl sulphoxide (DMSO) (0.1% final concentration) or with increasing amounts of Azaindole 1 (final concentration 0.1 nM-3 μM), the assays are initiated with [33P]ATP (3000 mCi/mmol) (10 μM). After 20 min incubation, the reaction is terminated by incubation at 95°C for 10 min. After centrifugation at 10 000 g for 1 min, an aliquot of each incubation is spotted on paper matts. The papers are dried and subsequently washed twice in distilled water. After being dried, the papers are coated with scintillator and counted for radioactivity. Inhibition curves are analysed by nonlinear regression using GraphPad Prism[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Male Wistar rats weighing 300-350 g are anaesthetized 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 in a solution of Transcutol/Cremophor EL/physiological saline (19/10/80 = v/v/v). 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Azaindole 1
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