A ROCK1 and ROCK2 inhibitor
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GSK269962

Item No. 19180

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yl]oxy]phenyl]-4-[2-(4-morpholinyl)ethoxy]-benzamide
CAS Number
850664-21-0
Synonyms
  • GSK269962A
  • GSK269962B
Molecular Formula
C29H30N8O5
Formula Weight
570.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 16 mg/mlDMF:PBS(pH7.2) (1:2): 0.3 mg/mlDMSO: 14 mg/ml
λmax
275 nm
SMILES
O=C(NC1=CC=CC(OC2=NC=C(N=C(C3=NON=C3N)N4CC)C4=C2)=C1)C(C=C5)=CC=C5OCCN6CCOCC6
InChi Code
InChI=1S/C29H30N8O5/c1-2-37-24-17-25(31-18-23(24)33-28(37)26-27(30)35-42-34-26)41-22-5-3-4-20(16-22)32-29(38)19-6-8-21(9-7-19)40-15-12-36-10-13-39-14-11-36/h3-9,16-18H,2,10-15H2,1H3,(H2,30,35)(H,32,38)
InChi Key
YOVNFNXUCOWYSG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $178

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    10 mg

    $312

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    25 mg

    $680

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    Product Description

    GSK269962 is a selective ROCK inhibitor with IC50 values of 1.6 and 6 nM for ROCK1 and ROCK2, respectively.1 It displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases.1 GSK269962 has been shown to block the generation of inflammatory cytokines in lipopolysaccharide-stimulated monocytes and to induce vasorelaxation in preconstricted rat aorta (IC50 = 35 nM).1 Oral administration of 1-30 mg/kg GSK269962 can dose-dependently lower blood pressure in spontaneously hypertensive rats.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Doe, C., Bentley, R., Behm, D.J., et al. Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J. Pharmacol. Exp. Ther. 320(1), 89-98 (2007).