ROCK-IN-2

SKU: orb1296196

Description

ROCK-IN-2

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 867017-68-3
• MW: 402.79
• Purity: 97.29% (May vary between batches)
• Formula: C₁₈H₁₃ClF₂N₆O
• SMILES: Cc1c[nH]c2nccc(Oc3c(F)cc(Nc4cc(Cl)nc(N)n4)cc3F)c12
• Target: ROCK
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:2 mg/mL (4.97 mM);DMSO:30 mg/mL (74.48 mM);H2O:Insoluble

Bioactivity

• Target IC50:
  ROCK2:1.1 nM (cell free)|ROCK1:0.6 nM (cell free)
• 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.
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• 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).
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• 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.
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Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Azaindole 1, Azaindole1, Azaindole-1, Inhibitor, inhibit, ROK, ROCKIN2, ROCK-IN-2, ROCK2, ROCK, ROCK1, ROCK IN 2, Rho-kinase, Rho-associated kinase, Rho-associated protein kinase, TC-S 7001, TC-S7001, TC-S-7001

Compound Identifiers

PubChem CID

11524200