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Catalog No. TQ0110   CAS 867017-68-3
Synonyms: Azaindole 1, TC-S 7001

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.

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ROCK-IN-2, CAS 867017-68-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 116.00
5 mg In stock $ 289.00
10 mg In stock $ 463.00
25 mg In stock $ 766.00
50 mg In stock $ 1,070.00
100 mg In stock $ 1,450.00
1 mL * 10 mM (in DMSO) In stock $ 392.00
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Purity: 97.59%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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 ROCK1:0.6 nM (cell free), ROCK2:1.1 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 Azaindole 1, TC-S 7001
Molecular Weight 402.79
Formula C18H13ClF2N6O
CAS No. 867017-68-3


Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

H2O: Insoluble

DMSO: 30 mg/mL (74.48 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Kast R, et al. Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase. Br J Pharmacol. 2007 Dec;152(7):1070-80. Epub 2007 Oct 15.

Related compound libraries

This product is contained In the following compound libraries:
Orally Active Compound Library NO PAINS Compound Library Cytoskeletal Signaling Pathway Compound Library Cell Cycle Compound Library Kinase Inhibitor Library Anti-Aging Compound Library Wnt/Hedgehog/Notch Compound Library TGF-beta/Smad Compound Library Inhibitor Library Neural Regeneration Compound Library

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ROCK-IN-2 867017-68-3 Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells ROCK inhibit Rho-kinase Rho-associated protein kinase Azaindole-1 ROCKIN2 Rho-associated kinase Inhibitor Azaindole 1 ROCK IN 2 Azaindole1 TC-S 7001 ROK inhibitor