GSK269962 is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 2 mg | In stock | $ 87 | |
| 4 mg | In stock | $ 147 | |
| 8 mg | In stock | $ 205 | |
| 20 mg | In stock | $ 401 | |
| 40 mg | In stock | $ 629 |
| Description | GSK269962 is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively. |
| Targets&IC50 | ROCK1:1.6 nM, ROCK2:4 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). |
| Synonyms | GSK 269962, GSK269962B, GSK269962A HCl |
| CAS No. | 850664-21-0 |
| Chemical Formula | C29H30N8O5 |
| Molecular Weight | 570.61 |
| Solubility | Ethanol: 6 mg/mL (9.88 mM) DMSO: 57.1 mg/mL(100 mM); H2O: <1 mg/mL |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
In vivo Formulation Calculator (Clear solution)Calculatorbottom
