[CAS NO. 2095432-71-4] GSK269962A HCl
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PRODUCTS SPECIFICATIONS [2095432-71-4]
Catalog
SLK-S7687
Brand
Selleck
CAS
2095432-71-4
DESCRIPTION [2095432-71-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 607.06 |
| Molecular Formula | C29H30N8O5.HCl |
| SMILES | O=C(NC1=CC=CC(OC2=CC3=C(N=C(C4=NON=C4N)N3CC)C=N2)=C1)C5=CC=C(OCCN6CCOCC6)C=C5.[H]Cl |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6473 mL | 8.2364 mL | 16.4728 mL |
| 5 mM | 0.3295 mL | 1.6473 mL | 3.2946 mL |
| 10 mM | 0.1647 mL | 0.8236 mL | 1.6473 mL |
| 50 mM | 0.0329 mL | 0.1647 mL | 0.3295 mL |
Description
GSK269962A HCl (GSK269962B, GSK269962) is a selective inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.
Targets
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.
References
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