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  2. ROCK
  3. ROCK-IN-2

ROCK-IN-2 (Synonyms: Azaindole 1; TC-S 7001)

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

ROCK-IN-2 (Azaindole 1; TC-S 7001) 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.

ROCK-IN-2 Chemical Structure

ROCK-IN-2 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  
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Based on 1 publication(s) in Google Scholar

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Description

ROCK-IN-2 (Azaindole 1; TC-S 7001) 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[1].

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

ROCK-IN-2 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. ROCK-IN-2 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. ROCK-IN-2 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

ROCK-IN-2 (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. ROCK-IN-2 (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. ROCK-IN-2 (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
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. ROCK-IN-2 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[1].

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

References
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Keywords:

ROCK-IN-2Azaindole 1TC-S 7001Azaindole1Azaindole-1ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKInhibitorinhibitorinhibit

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