Information GSK269962A HCl (GSK269962B, GSK269962) is a selectiveROCK(Rho-associated protein kinase)inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively. Targets ROCK1 (Cell-free assay); ROCK2 (Cell-free assay); MSK1 (Cell-free assay); RSK1 (Cell-free assay) 1.6 nM ;4 nM; 49 nM; 132 nM In vitro 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 μM 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-α protein production in macrophages. In vivo 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. Cell Research(from reference) Cell lines：Human primary smooth muscle cells Concentrations：3 μM Incubation Time：150 min
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
GSK269962A HCl
CAS number：2095432-71-4 molecular formula：C29H30N8O5.HCl
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | GSK269962B | GSK269962 | GSK 269962Benzamide,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]-,hydrochloride (1:1) | ||
| CAS number | 2095432-71-4 | molecular formula | C29H30N8O5.HCl |
| molecular weight | 607.06 g/mol | Exact mass | ≥98% |
| PSA | 156.000 Ų | logp | 3.776 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
