GSK269962A can potently inhibit ROCK enzymatic activity with IC50 values of 1.6nM and 4nM for ROCK1 and ROCK2 (measured by purified recombinant protein), respectively, also show inhibition against RSK1 and MSK1 with IC50 values of 132nM and 49nM. Pre-treatment with 3μM GSK269962A 30 minutes before AngII stimulation could inhibit the actin stress fiber formation induced by AngII in human primary aortic smooth muscle cells. Addition with GSK269962A into the tissue bath showed concentration-dependent relaxing effect with IC50 value of 35nM on contracted blood vessels induced by phenylephrine in vitro due to the inhibition of ROCK inhibition by GSK269962A. Oral administration of 0.3-3mg/kg GSK269962A dose-dependently reduced blood pressure in both SHR and DOCA-treated hypertensive rats. GSK269962A at concentration of 50nM could dramatically inhibit basal myometrial contraction at 72h and abolish the procontractile effect of LPS, but appeared to enhance LPS-induced secretion of IL-8 in PHM1-41 cells.
CAS Number: 2095432-71-4
Molecular Weight: 607.06
Chemical 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 hydrochloride
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 100 mg/mL(164.72 mM). Water: Insoluble.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
GSK269962A completely abolished the actin stress fiber formation induced by angiotensin II in human smooth muscles. Such suppressive effect on actin fiber formation was observed beginning at around 1 Î¼M GSK269962A. GSK269962A induced vasorelaxation in preconstricted rat aorta(tissue baths) with an IC50 of 35 nM. the relaxation induced by GSK269962A is reversible. GSK269962A suppressed IL-6 mRNA transcription and reduced LPS-induced IL-6 and TNF-Î± protein production in macrophages.
Oral administration of GSK269962A produced a profound dose-dependent reduction of systemic blood pressure in spontaneously hypertensive rats. The reduction of blood pressure was acute and substantial. The maximal effect on blood pressure was observed approximately 2 h after oral gavages. The reduction of blood pressure was accompanied by an acute, dose-dependent increase in heart rate, presumably due to the activation of baroreflex mechanism. ROCK inhibition with the use of GSK 269962 in the 10 mg/kg dose, in turn, triggered an increase in VV(voided volume), PVR(post-void residual), VT(volume threshold), VE(voiding efficiency), ICI(intercontraction interval), BC(bladder compliance), and VTNVC(volume threshold to elicit NVC). The inhibition of the ROCK pathway through GSK 269962 appeared to have no effect on either HR(heart rate), SBP(systolic blood pressure), MBP(systolic blood pressure), or DBP(diastolic blood pressure). NVC:nonvoiding contractions.
- Andrzej Wróbel, et al. Neurourology and Urodynamics. 2016.
- Doe C, et al. J Pharmacol Exp Ther. 2007, 320(1):89-98.
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