Azaindole 1

SKU: orb1217565

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.

Key Properties

• CAS Number: 867017-68-3
• MW: 402.79
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₃ClF₂N₆O
• SMILES: Cc1c[nH]c2nccc(Oc(c(F)cc(Nc3cc(Cl)nc(N)n3)c3)c3F)c12
• Target: ROCK
• Solubility: DMSO:30 mg/mL (74.48 mM; Need ultrasonic);Water:Insoluble

Bioactivity

• In Vivo:
  BAY-549 (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. BAY-549 (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. BAY-549 (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.
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• In Vitro:
  BAY-549 (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. BAY-549 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. BAY-549 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TC-S 7001 | ROCK-IN-2

Quick Database Links

Gene Symbol

ROCK