| Identification | Back Directory | [Name]
GSK269962A | [CAS]
850664-21-0 | [Synonyms]
CS-1126
GSK 269962
GSK269962B
GSK-269962 95%
GSK269962A(GSK269962)
GSK269962 (GSK269962A)
ROCK inhibitor GS269962A
ROCK inhibitor GSK269962A
GSK269962A ISO 9001：2015 REACH
GSK 269962A;GSK-269962A;GSK269962;GSK 269962;GSK-269962
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-morpholinoethoxy)benzamide
N-[3-[[2-(4-Aminofurazan-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yl]oxy]phenyl]-4-[[2-(4-morpholinyl)ethyl]oxy]benzamide
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 | [Molecular Formula]
C29H30N8O5 | [MDL Number]
MFCD09970310 | [MOL File]
850664-21-0.mol | [Molecular Weight]
570.6 |
| Chemical Properties | Back Directory | [Melting point ]
125 - 127°C | [density ]
1.45 | [storage temp. ]
under inert gas (nitrogen or Argon) at 2–8 °C | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
13.19±0.70(Predicted) | [color ]
Off-White |
| Hazard Information | Back Directory | [Description]
Two Rho-associated kinases (ROCKS), ROCK1 and ROCK2, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. GSK269962 is a selective ROCK inhibitor with IC50 values of 1.6 and 6 nM for ROCK1 and ROCK2, respectively. It displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases. 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). Oral administration of 1-30 mg/kg GSK269962 can dose-dependently lower blood pressure in spontaneously hypertensive rats. | [Uses]
GSK 269962 is a potent and selective Rho kinase (ROCK) inhibitor. | [in vivo]
GSK269962A is a potent antihypertensive agent. GSK269962A (0.3, 1, and 3 mg/kg; oral gavage) induces a dose-dependent reduction in blood pressure in spontaneously hypertensive rat (SHR). The reduction of blood pressure is acute and substantial[1]. | Animal Model: | Male Sprague-Dawley rats (350-400g)[1] | | Dosage: | 0.3, 1, and 3 mg/kg | | Administration: | Oral gavage; 12 hours | | Result: | Induced a dose-dependent reduction in blood pressure. |
| [IC 50]
ROCK1: 1.6 nM (IC50); ROCK2: 4 nM (IC50); RSK1: 132 nM (IC50); MSK1: 49 nM (IC50); AKT1: 955 nM (IC50); AKT2: 1350 nM (IC50); AKT3: 1510 nM (IC50); CDK2: 3500 nM (IC50); GSK3α: 1260 nM (IC50) | [storage]
Store at +4°C | [References]
[1] CHRIS DOE. Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 320 1: 89-98. DOI: 10.1124/jpet.106.110635 |
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